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July 2019 | Volume 32 Number 7 www.chromatographyonline.com PEER-REVIEWED ARTICLE Determining sulphonamides in liver LC TROUBLESHOOTING Mobile phase buffers in LC GC CONNECTIONS Temperature programmed GC Bioanalytical Method Validation Quantifying endogenously present small molecules in biological samples

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Page 1: Bioanalytical Method Validationfiles.alfresco.mjh.group/alfresco_images/pharma/2019/07/...2019/07/11  · Subscriber Customer Service Visit chromatographyonline.com to request or change

July 2019 | Volume 32 Number 7

www.chromatographyonline.com

PEER-REVIEWED ARTICLEDetermining sulphonamides in liver

LC TROUBLESHOOTINGMobile phase buffers in LC

GC CONNECTIONSTemperature programmed GC

Bioanalytical Method Validation

Quantifying endogenously present small molecules in biological samples

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are trademarks of Merck KGaA, Darmstadt,

Germany or its affi liates. All other

trademarks are the property of their

respective owners. Detailed information

on trademarks is available via publicly

accessible resources.

© 2019 Merck KGaA, Darmstadt, Germany

and/or its affi liates. All Rights Reserved.

To fi nd out more, visit:

SigmaAldrich.com/UnleashTheImpossible

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FEATURES

344 Sample Treatment in Routine Analysis: A Case

Study: Sulphonamides in Liver

Leah Walker, Francesc Borrull, Eva Pocurull, and Núria

Fontanals

A case study related to the determination of

sulphonamides in liver is presented. Different

extraction strategies, including solid-liquid extraction

(SLE), ultrasound-assisted extraction (UAE), and

solid-phase extraction (SPE), were evaluated to

produce a simple and effective extraction method.

COLUMNS

364 LC TROUBLESHOOTING

Mobile Phase Buffers in LC: Effect of Buffer

Preparation Method on Retention Repeatability

Dwight R. Stoll and Devin M. Makey

For liquid chromatography (LC) methods where the

buffer pH and composition have an influence on

retention, which buffer preparation method will provide

the most repeatable results?

370 GC CONNECTIONS

Temperature Programmed GC: Why Are All Those

Peaks So Sharp?

Nicholas H. Snow

Temperature programming is used for most

separations in capillary GC today. Despite this, many

of the principles by which we understand temperature

programmed capillary column separations are

based on ideas developed using packed columns

and isothermal conditions. This instalment of “GC

Connections” dives into temperature programming.

DEPARTMENTS

378 Products

380 Events

381 The Applications Book

Image credit: flashmovie/stock.adobe.com

COVER STORY

354 PHARMACEUTICAL PERSPECTIVES

Strategies for the Quantification of Endogenously

Present Small Molecules in Biological Samples

Maxim Nelis, Patrick Augustijns, and Deirdre Cabooter

The main objective of this review is to provide a

clear summary of the different methods that can

be used to quantify endogenous small molecules.

Practical recommendations to face this bioanalytical

challenge, in particular in terms of method

validation, will also be provided.

July | 2019

Volume 32 Number 7

342 LCGC Europe July 2019

CONTENTS

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Daniel W. Armstrong

University of Texas, Arlington, Texas, USA

Günther K. Bonn

Institute of Analytical Chemistry and Radiochemistry, University of Innsbruck, Austria

Deirdre Cabooter

Department of Pharmaceutical and Pharmacological Sciences, University of Leuven, Belgium

Peter Carr

Department of Chemistry, University of Minnesota, Minneapolis, Minnesota, USA

Jean-Pierre Chervet

Antec Scientific, Zoeterwoude, The Netherlands

Jan H. Christensen

Department of Plant and Environmental Sciences, University of Copenhagen, Copenhagen, Denmark

Danilo Corradini

Istituto di Cromatografia del CNR, Rome, Italy

Gert Desmet

Transport Modelling and Analytical Separation Science, Vrije Universiteit, Brussels, Belgium

John W. Dolan

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Anthony F. Fell

Pharmaceutical Chemistry, University of Bradford, Bradford, UK

Attila Felinger

Professor of Chemistry, Department of Analytical and Environmental Chemistry, University of Pécs, Pécs, Hungary

Francesco Gasparrini

Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università “La Sapienza”, Rome, Italy

Joseph L. Glajch

Momenta Pharmaceuticals, Cambridge, Massachusetts, USA

Davy Guillarme

School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, Geneva, Switzerland

Jun Haginaka

School of Pharmacy and Pharmaceutical Sciences, Mukogawa Women’s University, Nishinomiya, Japan

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Van’t Hoff Institute for the Molecular Sciences, Amsterdam, The Netherlands151 353 3601

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Monash University, School of Chemistry, Victoria, Australia

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Robert D. McDowall

McDowall Consulting, Bromley, Kent, UK

Mary Ellen McNally

DuPont Crop Protection, Newark, Delaware, USA

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Molnar Research Institute, Berlin, Germany

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Dipartimento Farmaco-chimico, Facoltà di Farmacia, Università di Messina, Messina, Italy

Peter Myers

Department of Chemistry, University of Liverpool, Liverpool, UK

Janusz Pawliszyn

Department of Chemistry, University of Waterloo, Ontario, Canada Colin Poole Wayne State University, Detroit, Michigan, USA

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Advanced Materials Technology, Chester, UK

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Research Institute for Chromatography, Kortrijk, Belgium

Pat Sandra

Research Institute for Chromatography, Kortrijk, Belgium

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Deakin University, Melbourne, Australia

Yvan Vander Heyden

Vrije Universiteit Brussel, Brussels, Belgium

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One of the current roles of analytical scientists is to determine low concentrations of

different compounds in complex matrices. The ability to quantify low concentrations

of compounds in an analytical method depends on the instrumental technique as

well as the sample preparation. In recent years, the sensitivity of detection

techniques has been improved by the development of mass spectrometry

(MS)-based detectors (1). However, sample preparation still plays a crucial role in

the development of an analytical procedure and is considered the most challenging

and variable step (2,3). The choice of sample treatment depends largely on the

matrix type, the method, and the physicochemical features of the analytes. The

typical steps involved in sample preparation include sampling, extraction, clean-up,

and concentration, followed by the final analysis (4). In addition, the development of

cost-effective analytical methods is a crucial factor for achieving versatile and

reliable results while largely avoiding the use of many high-tech instrumentation

resources that lead to an increase in the cost of the analysis.

An ideal extraction technique should achieve selective total extraction of the

target compounds (complete recoveries) while limiting the extraction of matrix

impurities. In addition, compromises are needed to ensure the technique is fast,

easy, and cheap as well as reducing organic solvent consumption. For solid

samples, among the most used extraction techniques are pressurized liquid

extraction (PLE), microwave-assisted extraction (MAE), and supercritical fluid

extraction (SFE). However, these techniques are all instrument-based and as such

have higher associated costs and not all laboratories have these instruments (5,6).

Traditional solid-liquid extraction (SLE) techniques are thought to be

time-consuming, lack efficiency in extracting target compounds, and require large

volumes of solvents. Nevertheless, this technique is still widely used because of

its simplicity and it does not require expensive equipment (5,6). As a result of

these features, this is often the only affordable technique available in laboratories

where routine analytical methods are developed.

Sample Treatment in Routine Analysis: A Case Study: Sulphonamides in LiverLeah Walker, Francesc Borrull, Eva Pocurull, and Núria Fontanals, Department of Analytical Chemistry and Organic Chemistry,

Rovira i Virgili University, Marcel·lí Domingo 1, Campus Sescelades, Tarragona, Spain

Currently, sample treatment is still the bottleneck in the development of analytical methods to analyze

complex samples, especially for routine analysis where high-tech instruments are not always available.

Research on the evaluation of different sample treatments is needed to achieve the sensitivity and selectivity

required. This article presents a case study related to the determination of sulphonamides in liver. Different

extraction strategies, including solid-liquid extraction (SLE), ultrasound-assisted extraction (UAE), and

solid-phase extraction (SPE), were evaluated to produce a simple and effective extraction method.

KEY POINTS• The role of sample treatment

is important when dealing

with complex samples.

• -Simple extraction techniques

are good alternatives to costly

instrumentation for some complex

samples such as edible tissues.

• -Sample treatment is still the

bottleneck in the development

of analytical methods.

344 LCGC Europe July 2019

FONTANALS ET AL.

PEER REVIEW

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It’s the DAWN of a new day.

Learn more at wyatt.com/NextGen

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Developments in classical SLE, where shaking by hand

usually ensures the partitioning of the analytes between the

solid matrix and the organic solvent, include sonication,

which is generally preferred to aid this contact between the

two phases and promote the extraction efficiency. This

extraction technique is known as ultrasound-assisted

extraction (UAE) (3,7).

Nevertheless, some studies have reported on the use of SLE,

not only for its simplicity, but also because it provided the best

extraction results. For instance, four common methods

(solid-phase extraction [SPE], matrix solid-phase dispersion

[MSPD], quick, easy, cheap, effective, rugged, and safe

[QuEChERS], and SLE) were compared and the authors found

that SLE followed by a clean-up step based on SPE using a

hydrophilic-lipophilic balanced copolymer SPE cartridge was

the most suitable approach for the simultaneous extraction of

antibiotics from eggs (8). Similarly, SLE was the extraction

technique of choice to extract a similar group of antibiotics

from swine manures (9). In another example (10), PLE and SLE

were compared for the extraction of a group of mycotoxins

from rat faeces. In this study, although the extraction efficiency

of PLE was higher, the authors finally developed the method

using SLE because it also provided suitable results, but the

method simplicity was an advantage when a large number of

samples had to be analyzed.

Among the different analytical methods where sample

preparation is important, the determination of veterinary

residues in edible tissues, such as the liver, was focused on

in this article. Antibiotics are widely administrated for

therapeutic purposes, but they can also be used for growth

promotion in food-producing animals. The use of antibiotics

for animal growth is considered fraudulent in Europe

because the residues of these compounds can persist in

edible matrices (11). For this reason, the European

Commission regulates their use through the establishment of

maximum residue levels (MRL) in foodstuff of animal origin

(12). Therefore, the presence of antibiotics in edible tissues

needs to be controlled through the development of analytical

methods in routine laboratories to comply with these

regulations.

With regards to sample preparation when working with

animal tissues, one of the main difficulties is related to the

complexity associated with the high fat and protein content in

these matrices (3,4). Thus, the sample preparation step is

critical in the development of the analytical method. In this

study, the general issue of affordable sample preparation for

routine analysis is transferred to the particular case of the

determination of antibiotics in liver tissue by presenting

different sample preparation strategies; however, these

strategies could be extended to other compounds present in

other complex matrices. The only constraint that is applied is

that these strategies should be simple and affordable to be

widely applied in any laboratory.

Experimental

Materials and Standards: Sulfadiazine (SDZ),

sulfamethoxazole (SMX), sulfamethazine (SMT), sulfapyridine

(SPY), sulfathiazole (STZ), all with purity ≥95%, ammonium

hydroxide solution (NH4OH), and formic acid were all

obtained from Sigma-Aldrich. HPLC-grade ethyl acetate

(EtAc), methanol, acetonitrile, and acetic acid (HAc) were all

purchased from J.T. Baker. Ultra-pure water was obtained

from a water purification system (Veolia Water). Individual

stock solutions of 1000 mg/L for each sulphonamide were

prepared in methanol and stored at 4 ºC. A standard working

solution of 100 mg/L was prepared weekly by diluting the

stock solutions with ultra-pure water and stored at 4 ºC. A

hydrophilic-lipophilic balanced copolymer and a mixed-mode

strong-cation exchange (SCX) polymer SPE cartridges of

150 mg format were used.

Sampling and Sample Treatment: Ovine liver samples were

purchased from local markets in Tarragona, Spain, and were

chopped and blended with a domestic food blender.

Homogenized samples were stored at -20 ºC prior to use. A

scheme highlighting the entire sample treatment and analysis

of the liver samples can be seen in Figure 1. Samples were

defrosted overnight at 4 ºC and a 1 g aliquot was transferred

into a 25-mL polypropylene centrifuge tube. The blank

FIGURE 1: Scheme of the optimized liver analysis procedure.

346 LCGC Europe July 2019

FONTANALS ET AL.

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and Canada.

Merck, the vibrant M and Supelco are trademarks of

Merck KGaA, Darmstadt, Germany or its affi liates. All

other trademarks are the property of their respective

owners. Detailed information on trademarks is available

via publicly accessible resources.

© 2019 Merck KGaA, Darmstadt, Germany and/or its

affi liates. All Rights Reserved.

For more information, please visit:

SigmaAldrich.com/SuccessReplicated

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samples were spiked when appropriate by adding the

working solution directly along with 10 mL of methanol. The

resulting solution was vortexed for 5 min using a vortex mixer

(Velp Scientifica) and then centrifuged at 1500 rpm for 10 min

using a Genevac miVac Duo Concentrator. The supernatant

was filtered using a 0.22-μm PTFE micro filter (Scharlab). The

resulting solution was made up to 10 mL again with methanol

and then diluted with water with 0.1% HAc to 50 mL. It was

then frozen at -20 ºC overnight to promote precipitation of

fats, lipids, and proteins. The solution was then centrifuged

for 25 min and filtered under gravity to obtain a clear solution

to submit to the mixed-mode SCX polymeric SPE cartridge for

clean-up and concentration of the sample. The SPE protocol

was as follows: the cartridge was conditioned with 5 mL of

methanol and then by 2 × 5 mL portions of ultrapure water.

The 50 mL sample solution was loaded and eluted with 10 mL

of 4.5% NH4OH in methanol. The solution was directly

injected into the LC–DAD system. During method validation,

the extract was evaporated to dryness using a Genevac

miVac Duo Concentrator, and reconstituted to 1 mL of mobile

phase.

LC–DAD Conditions: Chromatographic analysis was

performed using an Agilent 1100 HPLC system (Agilent

Technologies) equipped with a diode array detector (DAD), a

binary pump, and a 5 μL loop injector. Chromatographic

separation was performed using a 150 × 0.46 mm, 5-μm

Mediterranea Sea18 column (Technokroma). The mobile

phase was as follows: water with 0.1% HAc ~ pH 2.8 (A) and

acetonitrile (B). The flow rate was 1 mL/min, the monitoring

wavelength was 270 nm, and the column thermostat was set

at 30 ºC. The following gradient programme was used:

0–9 min from 10% to 55% (B); 9–11 min from 55% to 100%

(B); 11–15 min continued at 100% (B) and then returned to

initial conditions within 5 min.

Results and Discussion

Chromatographic Separation: Liquid chromatography (LC)

coupled to a DAD detector was used for chromatographic

separation, identification of analytes, and quantification. A DAD

detector can be used initially because, although it is not as

sensitive as MS, it is cheaper and more readily available, and if

necessary, the developed method can be easily transferred to

LC–MS because of the compatibility of the mobile phase. In

addition, sulphonamides absorb light in the UV–vis region and

the absorbance of the sulphonamides was evaluated from

220–360 nm. The monitoring wavelength was chosen to be

270 nm because this gave the strongest absorption for all

sulphonamides evaluated (13,14). The mobile phase chosen

was water with 0.1% HAc (A) and acetonitrile (B), which gave

adequate separation. To obtain sufficient retention and

separation, different elution gradients were tested and the

gradient that gave the best separation of compounds is

described in the experimental section. With this gradient all

compounds were eluted in 8 min.

When applied to liver samples, a high water content at the

beginning of the chromatographic run is needed to promote

the elution of interfering hydrophilic substances, co-extracted

from the complex liver matrix, in the first couple of minutes.

This avoids coelution with analytes and limits noise. Figure 2

shows a chromatogram where an extract from a liver sample,

spiked at 50 mg/kg with the analyte mixture, was injected. The

elution of various interferences can be seen in the first 5 min of

the chromatographic run. From 11–20 min after the gradient

had ended, the chromatographic run was continued at 100%

acetonitrile to clean the column and avoid a carry-over

phenomenon in the following chromatographic runs (15). While

this gradient provided the best possible separation, STZ and

SPY—the second and third eluted compounds—overlapped

slightly. However, resolution was calculated to be 1.87 ± 0.03

indicating they are sufficiently separated for this gradient

programme to be used.

Extraction Method: Animal tissues, particularly the liver, are

complex matrices that contain an abundance of interfering

components such as fats, proteins, and carbohydrates. However,

the liver is the site of detoxification and metabolism of

sulphonamides, which give a good indication of residue levels of

sulphonamides (16). To determine sulphonamides at low

concentrations, effective clean-up steps can be utilized rather than

increasing sensitivity through the use of expensive instrumentation.

SPE is a well-developed procedure used for clean-up and

concentration and is the most commonly used technique for food

and environmental sample preparation to determine veterinary

residues (17). Clean-up steps are essential in all samples and

must be optimized before the extraction technique.

60

50

40

30

20

10

0

mA

U

0 2.5 7.5 10

Time (min)

1512.5 17.5

SD

ZST

ZSP

Y

SM

T

SM

Z

5

FIGURE 2: The chromatographic separation of an extract from

a 1 g liver sample spiked with the five target sulphonamides at

50 mg/kg.

348 LCGC Europe July 2019

FONTANALS ET AL.

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Solid-Phase Extraction: Two different SPE cartridges were

evaluated for this procedure to concentrate the samples and

clean up the complex liver matrix: a hydrophilic-lipophilic

balanced copolymer SPE cartridge (150 mg), and a mixed-mode

SCX polymeric SPE cartridge (150 mg). They were evaluated

using initial conditions of 10 mL of aqueous solution spiked at

15 mg/L and eluting with 10 mL methanol. All these cartridges

have been previously used to retain sulphonamides so that

effective sample clean-up could occur; the hydrophilic-lipophilic

balanced copolymer SPE cartridge is the most popular for food

and environmental sample preparation for veterinary residues

(17–20).

Under the initial conditions, both cartridges gave full

recoveries of 92–130% for the mixed-mode SCX polymeric SPE

cartridge and 109–125% for the hydrophilic-lipophilic balanced

copolymer SPE cartridge. Previously, a silica-based modified

with C18 SPE cartridge was also evaluated, which provided

lower recoveries (35–90%) and had very poor reproducibility

with relative standard deviations (RSD) of between 15–30%.

Further optimization of both cartridges was achieved by

increasing the sample volume and by decreasing the elution

volume to concentrate the sample. For both cartridges, 50 mL

was chosen as the optimal sample volume as increasing the

sample volume up to this point did not affect recoveries. Larger

volumes than 50 mL were not evaluated since the loading

volume of SPE came from the extract for SLE. Moreover, 10 mL

was chosen as the elution volume because decreasing it from

10 mL to 5 mL resulted in some compounds not completely

eluting, in particular SDZ whose recoveries decreased by 37%

in the mixed-mode SCX polymeric SPE cartridge and 25% in the

hydrophilic-lipophilic balanced copolymer SPE cartridge. Two

TABLE 1: The percentage recoveries (n = 3) for the target sulphonamides with the hydrophilic-lipophilic balanced copolymer SPE

cartridge and mixed-mode SCX polymeric SPE cartridge when different loading solvents were tested using standard solutions

% Recovery

Hydrophilic-Lipophilic

Balanced Copolymer SPE

Cartridge

Mixed-Mode SCX Polymeric SPE Cartridge

H2O

0.1%HAc

Methanol/

H2O 0.1%

HAc (25:75)

H2O 0.1%HAc

Methanol/

H2O 0.1%

HAc (25:75)

Methanol

0.1% HAcMethanol EtAc

SDZ 103 43 90 65 37 17 11

STZ 116 52 117 114 87 35 48

SPY 128 68 130 106 133 118 69

SMT 120 86 106 111 50 32 17

SMZ 113 109 108 103 19 16 6

FIGURE 3: The percentage recoveries for each sulphonamide

when the hydrophilic-lipophilic balanced copolymer SPE

cartridge and the mixed-mode SCX polymeric SPE cartridge

were compared in SPE clean-up in a procedure starting from 1 g

of liver tissue spiked with the analyte mixture and including SLE,

and their associated % error (n = 5). H-L = hydrophilic-lipophilic.

FIGURE 4: The percentage recoveries for the target sulphonamides

when liver sample size was increased in the range 0.5 g to 5 g.

350 LCGC Europe July 2019

FONTANALS ET AL.

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different organic elution solvents were

tested, acetonitrile and methanol, and in

the case of the mixed-mode SCX

polymeric SPE cartridge, NH4OH was

added to displace ionic interactions. In

the mixed-mode SCX polymeric SPE

cartridge both organic solvents gave

similar recoveries, but the

hydrophilic-lipophilic balanced

copolymer SPE cartridge, methanol gave

increased (11–13%) recoveries for each

sulphonamide and was selected as the

extraction solvent in both cases.

As the loading solvent in SPE is the

extracting solvent in the previous SLE

step, solvents other than water were also

tested using standard solutions spiked at

15 mg/L for both SPE methods. The

mixed-mode SCX polymeric SPE

cartridge is a mixed mode sorbent

functionalized with sulfonic groups so

that it can establish cationic interactions

with the target analytes. Therefore,

organic solvent can be tested as the

loading solvent. In contrast for the

hydrophilic-lipophilic balanced

copolymer SPE cartridge, dilution of the

organic solvent with water or an

evaporation step must occur before SPE.

For this cartridge, dilution of methanol by

a factor of four was found to significantly

decrease recoveries, particularly for the

most hydrophilic compounds as shown

in Table 1. Therefore, an evaporation step

is needed after SLE to completely

remove the organic solvent and

reconstitute the sample in water to be

loaded into the hydrophilic-lipophilic

balanced copolymer SPE cartridge.

For the mixed-mode SCX polymeric

SPE cartridge, organic solvents

methanol, EtAc, methanol with 0.1%

HAc, and methanol–water with 0.1 HAc

(25:75) were tested to load analytes onto

the cartridge. Table 1 highlights that

EtAc, methanol, and methanol with 0.1%

HAc gave poor recoveries for SDZ, SMT,

and SMZ. Although water with 0.1% HAc

gave the highest percentage recoveries,

25:75 methanol–water with 0.1% HAc

was chosen as the loading solvent

because it gave similarly good

recoveries, bar slightly lower for SDZ,

and disregards the need for an

evaporation step of the extract from SLE.

The recoveries and standard error for

the two optimized SPE methods when

applied to a 1 g liver sample spiked at

150 mg/kg, including the SLE extraction

step of 10 mL methanol and 5 min

extraction time, can be seen in Figure 3.

For the hydrophilic-lipophilic balanced

copolymer SPE cartridge, the resulting

solution from SLE was evaporated to

dryness and reconstituted in 50 mL of

water. SPE clean-up was performed and

compounds were eluted with 10 mL of

methanol. For the mixed-mode SCX

polymeric SPE cartridge, the resulting

solution from SLE was diluted to 50 mL

with water with 0.1% HAc (final solution

was 25:75 methanol–water v/v) before

SPE clean-up where compounds were

eluted with 10 mL of methanol with 4.5%

NH4OH. The mixed-mode SCX

polymeric SPE cartridge was chosen

because recoveries were higher with the

exception of SDZ. In addition, this

procedure is less time consuming than

that of the hydrophilic-lipophilic

balanced copolymer SPE cartridge due

to the absence of an evaporation step.

Solid-Liquid Extraction: Although PLE

can be used to extract analytes from the

solid matrix, it is expensive and

unavailable in routine laboratories.

Therefore, SLE with UAE and manual

extraction were tested for the extraction

of compounds from the liver. As SPE

conditions were optimized before SLE

conditions, methanol was chosen as the

extraction solvent because it provided

the best recoveries in SPE; no other

organic solvents were tested. Thus, in

both cases, 10 mL of methanol was

added to 1 g of liver and the resulting

mixture was shaken or sonicated for

5 min. The resulting solution was

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subjected to the optimized SPE clean-up procedure as the

sample is too complex to be analyzed at this stage. The

recoveries obtained are in general those depicted in Figure 3,

with values ranging from 82% to 105% for all the compounds,

with the exception of SDZ (56%).

Increasing the extraction time for longer than 5 min was

found to have no effect on recoveries. Decreasing methanol

volume from 10 mL to 5 mL resulted in lower recoveries (from

97% to 49%); therefore, methanol volume was kept at 10 mL.

Recoveries obtained for UAE and manual extraction aided

with vortex were similar, between 61–106%. As a result,

manual extraction was chosen as a more readily available

method as UAE equipment was deemed unnecessary.

To lower the limits of detection (LOD), sample size can be

increased. However, increasing sample size also increases

the amount of interfering matrix components. Liver sample

size was increased from 0.5 g to 5 g to test the optimal

amount. A 1 g sample of liver gave good recoveries

(60–100%); however, when the liver amount was increased to

1.5 g, the recoveries were lower (49–97%) as seen in

Figure 4. Therefore, 1 g of sample was selected.

After SLE extraction with methanol, the sample was diluted

with water prior to SPE extraction. However, this promoted

the precipitation of fats and proteins. “Freezing-out” of

interfering components was a simple and cheap method

utilized by freezing extracts overnight and centrifuging for

25 min to remove interfering fats and proteins and provide a

cleaner extract. Although this step is long, it allows many

samples to be treated simultaneously.

The final optimized method consisted of taking 1 g of liver,

adding 10 mL methanol, and vortexing for 5 min. The

solution was then centrifuged and the supernatant was

filtered with a 0.22-μm PTFE filter and made up to 10 mL

again with methanol before diluting to 50 mL with water with

0.1% HAc. This solution was frozen overnight, centrifuged for

25 min, and then filtered under gravity to obtain a clear

solution percolated in the mixed-mode SCX polymeric SPE

cartridge. The SPE protocol was as follows: the cartridge

was conditioned with 5 mL of methanol and then by 2 × 5 mL

portions of ultrapure water. The 50-mL sample solution was

loaded and eluted with 10 mL of 4.5% NH4OH in methanol.

The solution was directly injected into the LC–DAD system.

To further decrease the limits of detection, an evaporation

step can occur after elution. This strategy was only used in

the method validation. However, during the method

optimization, samples were directly injected from the eluted

10 mL of 4.5% NH4OH in methanol because this is quicker

and more straightforward than when it needed to be

evaporated.

Method Validation: The final method was validated to

demonstrate its performance by assessing linearity,

percentage recoveries, repeatability, reproducibility, LODs,

and limits of quantification (LOQ).

Instrumental calibration curves were first constructed from

standard solution and good linearity from 0.05 or 0.1 mg/L to

30 mg/L was found for all analytes, with the value for the

coefficient of determination (R2) being above 0.996 in all

cases.

The final percentage recoveries were calculated by spiking

the 1 g liver samples at 1 mg/kg and using the optimized

procedure. Table 2 shows recovery values ranging from 78%

to 99% with the exception of SDZ (64%). All RSDs were

below 10% showing highly reproducible results. It should be

mentioned that a non-spiked liver sample was first analyzed,

and peaks at the same retention time to the target analytes

were subtracted.

Method limit of quantification (MQLs) were calculated by

applying the percentage recoveries as well as the

concentration factor to the lowest point on the calibration

curve. Method limit of detection (MDLs) were calculated by

dividing this value by three and then subsequently spiking

samples to obtain this final concentration to show that it is

identifiable. Signal-to-noise ratio (S/N) criterion higher than

three and 10 was used for MDLs and MQLs, respectively. All

these results are displayed in Table 2.

The repeatability and reproducibility of the method were

evaluated using five replicate extractions of 1 g of liver

sample spiked at 2×MQL and performed on the same day or

on different days, respectively. Both were expressed in terms

of %RSD, which was 8–18% for repeatability and 9–29% for

reproducibility.

As the MDL values obtained were 0.01–0.05 mg/kg, which

is below the total MRL of 0.1 mg/kg for all sulphonamides

issued by the EU Commission, this method can be used to

TABLE 2: Validation parameters for each sulphonamide when

applied to 1 g liver samples

% Ra MQL (mg/kg) MDL (mg/kg)

SDZ 64 0.1 0.05

STZ 83 0.1 0.02

SPY 99 0.1 0.02

SMT 78 0.05 0.01

SMZ 79 0.05 0.01

a %R calculated when 1 g of liver sample was spiked at 1 mg/kg with the mixture

of the target sulphonamides. See the text for the experimental conditions. RDS (n

= 5) < 10%.

352 LCGC Europe July 2019

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confirm EU regulations are conformed

to and it can also easily be transferred

to LC–MS to lower MDLs.

Conclusions

Although a more sensitive technique,

such as tandem mass spectrometry

(MS/MS), can be used to obtain lower

MDLs, this technology is not always

available in routine laboratories. With

respect to sample extraction, in this

case it was found that cost could be

cut by using more basic techniques,

such as UAE and conventional SLE

methods, which gave good recoveries,

rather than methods using more

expensive instrumentation, such as

PLE and MAE.

It is evident that the complexity of the

animal matrix is still creating a huge

problem to produce effective methods

to routinely comply with EU regulations.

Finding effective sample clean-up and

extraction techniques to reduce

interfering matrix components is still an

area open for improvement and

exploration.

Acknowledgements

The authors would like to thank the

Ministerio de Economía y

Competitividad and the European

Regional Development Fund (ERDF)

(Project: CTQ2017-84373-R and

CTQ2017-88548-P) for the financial

support given.

References1) J. Aceña, S. Stampachiacchiere, S. Pérez, and D.

Barceló, Anal. Bioanal. Chem. 407, 6289–6299

(2015).

2) L. Ramos, J. Chromatogr. A 1221, 84–98 (2012).

3) M. Núñez, F. Borrull, N. Fontanals, and E.

Pocurull, Trends Anal. Chem. 97, 136–145

(2017).

4) M. Pérez-Rodríguez, R. Gereado Pellerano, L.

Pezza, and H. Redigolo-Pezza, Talanta 182,

1–18 (2018).

5) A. Larivière, S. Lissalde, M. Soubrand, and M.

Casellas-Français, Anal. Chem. 89, 453–465

(2017).

6) P. Vázquez-Roig and Y. Picó, Trends Anal. Chem.

71, 55–64 (2015).

7) B.K. Tiwari, Trends Anal. Chem. 71, 100–109

(2015).

8) A.G. Frenich, M.D. Aguilera-Luiz, J.L.M. Vidal,

and R. Romero-González, Anal. Chim. Acta 661,

150�160 (2010).

9) M. Solliec, A. Roy-Lachapelle, and S. Sauvé, Anal.

Chim. Acta 883, 415–424 (2015).

10) E. Miró-Abella, P. Herrero, N. Canela, L. Arola,

M.R. Ras, F. Borrull, and N. Fontanals, J.

Chromatogr. B 1105, 47–53 (2019).

11) A. Freitas, J. Barbosa, and F. Ramos, J.

Chromatogr. B 976, 49–54 (2015).

12) European Commission, O� . J. Eur. Union L15,

1–72 (2010).

13) Q. Zou, M. Xie, Y. Liu, J. Wang, J. Song, H. Gao,

and J. Han, J. Sep. Sci. 30, 2647–2655 (2007).

14) K. Deng, X. Lan, G. Sun L. Ji, and X. Zheng, Food

Anal. Methods 9, 3337–3344 (2016).

15) M.T. Martins, J. Me, F. Barreto, R.B. Ho� , L. Jank,

M.S. Bittencourt, J.B. Arsand, and E.E.S.

Schapoval, Talanta 129, 374–383 (2014).

16) H. Abdallah, C. Arnaudguilhem, F. Jaber, and R.

Lobinski, J. Chromatogr. A 1355, 61–72 (2014).

17) A. Andrade-Eiroa, M. Canle, V. Leroy-Cancellieri,

and V. Cerdà, Trends Anal. Chem. 80, 641–654

(2016).

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1289–1296 (2014).

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333–337 (2007).

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Food Chem. 83, 601–608 (2003).

Leah Walker is currently completing

her MChem degree at the University

of Edinburgh.

Francesc Borrull is Full Professor

in analytical chemistry in the

Analytical and Organic Chemistry

Department at the Rovira i Virgili

University in Tarragona since 2003.

Eva Pocurull is Assistant Lecturer

in analytical chemistry in the

Analytical and Organic Chemistry

Department at the Rovira i Virgili

University in Tarragona since 2000.

Núria Fontanals is Senior

Researcher in the Analytical and

Organic Chemistry Department at

the Rovira i Virgili University in

Tarragona since 2007.

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Strategies for the Quantifi cation of Endogenously Present Small Molecules in Biological SamplesMaxim Nelis, Patrick Augustijns, and Deirdre Cabooter, University of Leuven, Department of Pharmaceutical and Pharmacological

Sciences, Leuven, Belgium

The quantification of endogenously present compounds in biological samples demands appropriately validated

methods, in particular because increasing research efforts are aimed at studying the impact of such compounds

on human health and disease. International regulatory agencies, such as the Food and Drug Administration (FDA)

and the European Medicine Agency (EMA), have published a vast number of guidelines concerning bioanalytical

method validation over recent decades. Compared with the quantification of exogenous compounds, these

guidelines have remained rather vague and unclear when it comes to the quantification of endogenous compounds.

Nonetheless, the continuous expansion of studies devoted to the search for endogenous disease markers in the

human metabolome has incited the regulatory bodies to include endogenous compounds in a draft of an updated

International Conference on Harmonization (ICH) guideline on bioanalytical method validation. In light of these recent

developments, the main objective of this review article is to provide a clear summary of the different methods that

can be used to quantify endogenous small molecules. Because of the increased use of mass spectrometry (MS) in

the field of bioanalysis, a special focus will be placed on quantification by liquid chromatography (LC)–MS. Practical

recommendations to face this bioanalytical challenge, in particular in terms of method validation, will also be provided.

Endogenous analytes serve as important upstream

indicators and informative sources for downstream

biological processes (1). Apart from providing a platform

for the in-depth understanding of the underlying molecular

mechanism of a disease, metabolites might also play key

roles as “biomarkers” in the early diagnosis and prognosis

of diseases. The surge in high resolution and sensitive

mass spectrometry (MS) instruments has tremendously

propelled the realm of metabolomics and, hence, the

human metabolome has received increased attention as a

major source of information related to health and disease.

Nonetheless, a reliable quantification, in terms of accuracy

and precision, is hampered by the lack of a true blank

matrix, that is, a matrix without the analyte of interest, in

order to prepare matrix-matched calibrators (2). The use of

matrix-matched calibrators is recommended in the analysis of

biological samples, particularly when a mass spectrometer is

used. This is because matrix effects (MEs) are likely to occur

in the ionization source that might result in false negative and

false positive diagnostics (3,4,5). An additional challenge

lies in the absence of samples with a priori known quantities

of the compound of interest, which are required to check

for the accuracy of the method and the determination of the

quantitation limit. Even though the most recent Food and Drug

Administration (FDA) guidelines (2018) on bioanalytical method

validation address the challenge related to the quantification

of endogenous compounds, they merely provide some

general advice on the use of analyte-free matrix and the need

to evaluate parallelism (6). The Japanese Ministry of Health,

Labour, and Welfare (MHLW) recognizes the use of a surrogate

matrix on condition that its validity has been shown, but it does

not specify any further practicalities (7). The European Medicine

Agency (EMA), on the other hand, does not provide any

considerations on endogenous compounds in its guidelines (8).

Nonetheless, very recently, a joint effort of these three regulatory

bodies in the International Conference on Harmonization (ICH)

has resulted in a draft version of bioanalytical guidelines, which

now addresses the issue of endogenous compounds (9). The

respective regulatory agencies are accepting comments

until September 2019 before its formal implementation.

Over the years, three major strategies have been proposed

to quantify endogenous compounds: (i) the standard addition

method (SAM), (ii) quantification in a surrogate matrix, and (iii)

quantification with a surrogate analyte. As well as these, the

use of background subtraction has also been suggested. In

the latter, the calibration curve is created by spiking authentic

matrix with increasing concentrations of the compound of

interest. The resulting response curve is subsequently corrected

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15

Psilocin

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for the endogenous (background) signal of the compound of

interest in the original matrix. Since the quantification limit is

confined by the endogenous levels and is consequently larger

than in other methods, the use of background subtraction has

remained limited (10). Nonetheless, correction of the resulting

peak area for background signal can serve as a viable way

to deal with the insufficient removal of the compound from the

matrix by, for instance, charcoal treatment (11). Each of the

approaches mentioned is associated with practical challenges,

advantages, and drawbacks, which are discussed in the

first part of this review. In the second part, further potential

issues related to the validation of the analytical method will be

addressed, including the determination of linearity, parallelism,

accuracy, matrix effects, and the limit of quantification.

Quantifi cation Strategies

Standard Addition Method: The standard addition method

(SAM) is recommended when no internal standards (IS) are

available to compensate for pronounced matrix effects. In

particular in multicomponent analysis, finding an adequate IS

for each analyte is not always possible. The standard addition

method comprises the addition of a reference standard of

the analyte of interest at increasing concentration levels into

multiple aliquots derived from the same biological sample

in which the endogenous concentration of the analyte has

to be determined. One aliquot remains unspiked. After

analysis, the detector response is plotted against the added

concentration and the endogenous concentration is derived

from the negative intersection with the x-axis (Figure 1). As

an alternative, the concentration can be plotted against the

detector response and the endogenous concentration can

be obtained from the intersection with the y-axis, which can

be immediately derived from the regression equation. This is

referred to as the reversed-axis method (Figure 1) (12,13).

SAM considers matrix effects by relying on the assumption

that all concentration levels—both endogenous and spiked—

experience a proportional ion enhancement or suppression

effect because each aliquot contains the same amount of

coeluting matrix compounds. As a new calibration line is

created for each individual sample, the method also considers

inter-individual differences in matrix effects. The use of SAM

has remained rather limited in the liquid chromatography–mass

spectrometry (LC–MS) analysis of biological samples because

matrix effects are mostly compensated by the use of an

appropriate IS (14) (see section “Surrogate Matrix Approach”).

The use of extrapolation presumes that the relationship

between the concentration and the response remains

unchanged outside the linear range. Therefore, the spiked

concentration range should be as close as possible to the

endogenous levels. The EU guideline on pesticide analysis,

a field where SAM is more commonplace, prescribes that

the added amounts should be within one half and five times

the endogenous concentration (15). However, this requires

information on the endogenous concentration levels, which

is, of course, the question of interest. To deal with this, an

explorative study needs to be conducted. One possible

method regards the estimation of these levels using an

external calibration curve created in solvent (16). Nevertheless,

it is doubtful whether the concentration obtained by this

method can serve as a trustworthy prediction because of

the occurrence of matrix effects, which, moreover, might also

vary between samples. As an alternative, a certain number

of samples can be spiked at a wide range of concentration

levels. After choosing an appropriate calibration model to fit

the data, the curve can be extrapolated to a tentative value

for which the subsequent spiking levels are selected, at for

instance 0.5, 1, and 2 times the tentative value. The remaining

spiking levels are omitted and the curve is again extrapolated

to zero response. Once the average expected endogenous

concentration is established, the remaining samples can be

spiked with a lower number of spiking levels, which cover

approximately 0.5, 1, and 2 times the expected level. This

approach was used by Olesti et al. (16) and resulted in values

that did not differ more than 15% from those obtained by

employing the surrogate matrix approach with the inclusion

of an IS (see section “Surrogate Matrix Approach”).

Even though the use of an IS is not required to compensate

for matrix effects, recent work by Hewavitharana et al. (2018)

has shown that the addition of an internal standard can

successfully correct for procedural errors and variations in

instrumental response (13). They showed that the IS can

even be used to correct for other compounds, provided

that the response of the internal standard is not influenced

by its unlabelled counterpart. This method was proven to

be superior to the use of an IS as surrogate analyte.

Surrogate Matrix Approach: The most widely adopted

way to quantify endogenous components in biological

FIGURE 1: The reversed-axis method (right) as an alternative

for the conventional way (left) to determine the endogenous

concentration by using SAM.

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samples is by using a surrogate matrix. This approach

is often called isotope dilution and involves the use of

the authentic analyte in an analyte-free matrix in order

to prepare the calibration standards. The endogenous

concentration is then simply calculated from the calibration

curve by interpolation. Surrogate matrices cover a broad

range of alternatives for the original matrix going from its

most simple form, a solvent or buffer, to more complex

alternatives including so-called stripped matrices in which

the analyte has been removed from the matrix (17–20).

Even though the method is simple and straightforward, it

is important to recognize that the matrix effects exercised

on the analyte might differ considerably in the authentic and

surrogate matrix. Even when the samples are subjected

to an extensive sample clean-up, such as solid-phase

extraction (SPE), matrix effects might still be pronounced

(5,21). Therefore, an IS can be added to both the calibrators

and the samples at a fixed concentration. The general idea is

that the IS experiences the same matrix effect as the analyte

of interest and, hence, their peak areas are affected to the

same degree. Regardless of any matrix effect, the analyte

to IS peak ratio will thus remain unaffected. For a given

concentration, the following equation (equation 1) then applies:

Analyte

Matrix Surrogate matrix

=IS

Area

Area

Analyte

IS

Area

Area

[1]

In order to experience the same matrix effect, the natural

analyte and its IS should have the same retention time and

similar physicochemical properties. A stable isotopically

labelled internal standard (SIL-IS) is considered the best

option due to its structural relatedness with the nonlabelled

analyte. The difference in mass generated by isotopic labelling

provides the option to differentiate the structural analogues

using MS. However, given the natural abundance of isotopes,

the SIL-IS should differ at least three mass units from its

nonlabelled analogue in order to minimize spectral overlap (22).

Despite its structural similarity, a SIL-IS does not always

guarantee successful compensation for the matrix effect

experienced by a target compound. The replacement of a

carbon-hydrogen bond by a carbon-deuterium bond, for

example, might decrease the polarity of the molecule and

affect its retention time. This phenomenon is known as the

isotope effect and can be circumvented by employing 13C or 15N labelled internal standards or by altering the

chromatographic conditions (23,24). Regarding which

concentration of IS to add, it is vital to investigate the influence

of the concentration of both IS and target analyte on each

other’s ionization signal in advance. A suitable IS concentration

should be selected to keep the product of the peak area

ratio (analyte/IS) and the inverse of the analyte concentration

(equation 2) constant across the entire linear range (25):

Constant = Response 1

xResponse [Analyte]IS

Analyte

[2]

Apart from compensating for matrix effects, the use of

SIL-ISs offers other advantages. It considers inter-individual

differences since the response ratios at a certain concentration

will not differ from sample to sample, even though the

matrix effect might be present to a different extent (21). A

SIL-IS can also compensate for other variable parameters

that might affect accurate and precise quantification, such

as procedural errors during sample clean-up (21,25,26).

Nevertheless, it is important to always assess whether analyte

and SIL-IS possess equal extraction recoveries (27–29).

Notwithstanding these advantages, the choice for

a SIL-IS might be restrained as a result of economic

reasons or commercial unavailability, particularly in

multicomponent analysis. In this case, the standard

addition method might be a viable alternative.

Surrogate Analyte Approach: In this approach, the calibration

curve is created in authentic matrix by using a surrogate

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analyte possessing an identical ionization behaviour as the

naturally occurring compound. This is a stringent requirement

as both compounds should produce identical peak areas at

each concentration level to generate accurate results. For this

reason, a response factor (RF), expressing the difference in

peak area at the same concentration, is generally calculated

(equation 3) (28,30–31). Because of the endogenous nature

of the analyte, the RF can only be calculated in neat solution.

The RF should ideally be equal to 1 and can be optimized

by altering the collision energy in the MS instrument (28).

Alternatively, a correction factor reflecting the average RF at

different physiologically relevant concentration levels should be

included in the final calculation (equation 4) (17,31). The RF is

sometimes omitted in the final calculation of the endogenous

concentration if the difference in response is not greater

than 5% (28,32). The RF should be checked regularly after

optimization because changes in ionization efficiency might

occur, for example,after shutdown of the instrument (30).

RF =Response

Response

natural analyte

surrogate analyte

[3]

Regarding the choice of the surrogate analyte, a labelled

analogue offers the best option given its structural similarity

with its natural counterpart and, hence, similar ionization

behaviour. Moreover, since the surrogate analyte does not

consider matrix effects, an IS, correcting for the matrix effects

experienced by the natural as well as the surrogate analyte,

must be added as well. This triangular relationship demands a

strong compatibility between natural analyte, surrogate analyte,

and IS for which labelled analogues are the best choice. In this

case, the mass of all the analogues should differ sufficiently

to prevent overlap of their respective isotopic pattern.

The endogenous concentration is calculated

in accordance with the following formula:

[(Response

m

surrogate analyte/ IS) x RF ] –bConcentration =natural analyte

Response

[4]

in which m represents the slope of the calibration curve,

b its y-intercept, and RF the average response factor.

Validation

Regression Analysis and Parallelism: The calibration

range should comprise a physiologically relevant range

wherein at least six equally distributed concentration levels

are included (33,8). Although EMA and FDA do not compel

the replicate analysis of each calibrator, it is advised to

perform at least duplicate analysis at each level (6,8,34).

The choice of an appropriate regression model is necessary

to ensure accurate results. To fit the data to a linear curve, the

ordinary least squares regression (OLS) method is the simplest

approach in bioanalysis. The OLS method assumes that the

response variables have equal variances across the entire

concentration range, often referred to as homoscedasticity

(35). To verify this, the residuals can be plotted against the

concentration (34). In case of homoscedasticity, the residuals

will be homogenously distributed around the x-axis. Another

fast approach comprises the computation of the F-value,

which represents the ratio of the highest to the lowest variance

(36–38). This calculated F-value is compared against the critical

F-value to evaluate whether the assumption is violated or not.

In case of unequal variances, the number of calibration

points can be decreased because higher variances are often

observed at higher concentrations. This can only occur at the

cost of a reduction of the interpolation range (36). When SAM

is used, the highest spiked values can be eliminated, provided

that a sufficient amount of calibration points remain to assess

linearity. Alternatively, a weighed linear regression (WLS) model

can be applied (37). In bioanalysis, the following empirical

weighing factors are commonly used: 1/x, 1/x², 1/y, and 1/y². To

verify which weighing factor is appropriate, the back-calculated

FIGURE 3: Determining accuracy when the surrogate matrix or

surrogate analyte approach is used (left) and when SAM is used

(right). The arrow indicates the difference between CM and C

0

that should be compared with the nominal spiked concentration.

FIGURE 2: Calibration curve in authentic matrix with surrogate

analyte or in surrogate matrix with authentic analyte showing

parallelism with matrix 1, but not with matrix 2.

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concentrations of the calibrators should be compared with the

nominal values. The relative residual (equation 5) should be

within 15% for at least 75% of the calibration levels (6,8,16,37):

x 100%Relative residual (%) =

Conc –Concback–calculated

Concnorminal

nominal

[5]

If linear regression models are not sufficient to fit the data

across the desired concentration

range, polynomial regression

models can be considered. Note

that the addition of an increasing

number of independent variables will

automatically result in an increased

coefficient of determination (R²).

Even though it is often used as a

criterion to gauge the goodness

of fit of the calibrator data, an

increased R²-value might also be

the result of overfitting and, hence,

does not necessarily imply a higher

predictive power. Therefore, other

formal tests to assess whether an

increase in prediction parameters

improves the fitting are more

suitable, such as the lack-of-fit test

(LOF) or Mandel’s test (39–41). In

accordance with Occam’s razor,

the simplest model describing the

relationship is always preferred (6).

Because the detector

response might be different in

matrix and solvent, international

guidelines advocate the use of

matrix-matched calibrators. Strictly

speaking, the standard addition

method encompasses the use of

matrix-matched calibrators because

a calibration curve is created

in each individual sample (13).

Nonetheless, it is necessary to be

aware that SAM assumes a linear

relationship outside the calibration

range and as aforementioned, it is

for this reason required to evaluate

linearity as close as possible to the

endogenous concentration value.

The surrogate analyte approach

involves the use of authentic

matrix to create the calibration curve. However, it must

still be verified whether matrix effects experienced by

the authentic and surrogate analyte are equal. This

can be examined by showing so-called parallelism

(28,42). From a practical point of view, a matrix spiked

with authentic analyte at increasing levels is compared

with the same matrix spiked with increasing levels of

the surrogate analyte (Figure 2). The IS is added at a

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fixed concentration level each time to correct the peak

area of authentic and surrogate analyte. If the obtained

slopes of the calibration curves do not differ significantly

from each other, parallelism has been demonstrated.

Significance can be traced by a formal t-test (43).

In contrast with SAM and the surrogate analyte

approach, the surrogate matrix approach does not involve

the creation of the calibration curve in authentic matrix. In

this case, demonstrating parallelism between the authentic

and surrogate matrix is necessary to ensure the valid use

of a surrogate matrix (43,44). Both authentic and surrogate

matrix are for this purpose spiked at increasing levels of

the analyte and at a fixed level of the IS. The regression

curves are compared as described above (Figure 2).

Accuracy: Accuracy is a measure to describe the trueness

with which the concentration is determined in samples

(quality controls [QCs]) containing known amounts of

analyte, that is, the nominal amount. The concentration is

determined against the calibration curve and the accuracy

value is expressed as the ratio of the determined value

to the nominal value. The accepted deviation from the

nominal value is set at ± 20% for the LLOQ and ± 15% for

higher levels. However, as the endogenous concentration

is unknown, the accuracy of the method cannot be

assessed in this way for endogenous compounds. This

hiatus can be bypassed by using equation 6, in which

CM represents the measured concentration upon spiking,

C0 the measured basal concentration level, and C

s

the nominal spiked concentration (Figure 3) (45):

Accuracy (%) = x 100%C 0–CM

C S [6]

Both CM and C

0 are determined using either one of the

suggested methods in the ”Quantification Strategies” section.

Since the physiologically relevant range might be

surpassed by spiking the authentic matrix, the draft version

of the ICH bioanalytical guidelines recommends the use

of QC samples with the lowest endogenous concentration

(9). Besides stating that the spiked concentration levels

should be statistically different from the endogenous

concentration, it does not provide any further requirements

regarding spiking concentrations. However, it should be

recognized that spiking outside a physiologically relevant

range might undermine the actual accuracy of the method.

Therefore, spiking levels are suggested to not exceed

four times the expected endogenous concentration (46).

The determination of accuracy through spiking

might also enable to demonstrate the validity of the

utilization of the surrogate matrix or surrogate analyte

for quantification purposes as accuracy values within

predefined limits justify their usage (9,17,32,42).

Contrary to SAM and the surrogate matrix

approach, the surrogate analyte approach enables

the accuracy of the method below the natural

endogenous level to be monitored by using the

surrogate analyte to prepare QCs (30).

Matrix Effect: The matrix effect can be calculated in

multiple ways. EMA suggests the calculation of a matrix

factor (MF) (8). This parameter compares the response

of the analyte spiked at the same concentration level in

authentic matrix and in neat solution. In case the sample

undergoes a pretreatment step, the analyte is spiked

in the extracted matrix to differentiate the matrix factor

from recovery (47,48). The method is often referred to

as the post-extraction spike method (48). To circumvent

interfering responses arising from basal analyte levels,

the peak area of the unspiked matrix is subtracted from

the peak area of the spiked matrix (equation 7) (29,47):

MF =Analyte

Peak Area (Analyte Spiked in Matrix)– Peak Area (Endogenous Analyte in Matrix)

Peak Area (Analyte in Pure Solution)

[7]An MF < 1 indicates ion suppression and an

MF > 1 indicates ion enhancement with respect

to the response of the analyte in neat solution.

The IS should experience the same matrix effect as the

analyte of interest in order to function as an appropriate IS.

The matrix factor of the IS can be calculated without any

correction for endogenous levels (equation 8) (8,17,29).

MF =IS

Peak Area (IS in Matrix)

Peak Area (IS in Pure Solution) [8]

By dividing the MF of the analyte with the MF of the IS,

the IS-normalized MF is calculated. In spite of the absence

of any limits provided by the regulatory agencies, the

normalized MF should be as close to unity as possible.

The inter-individual variability of the IS-normalized MF,

often referred to as the relative matrix effect, should be

assessed by analyzing a minimum of six different samples.

The variability of the matrix effect among the samples

is expressed in terms of covariance and should not

exceed the limit of 15% (8). More stringent cut-off values

(CV < 5%) have, however, also been put forward (48,49).

Alternatively, the matrix effect can be assessed by

comparing the slopes of a standard addition curve in

matrix with a standard curve in neat solution, both spiked

at equal concentration levels posterior to the sample

preparation step (49,50). Slopes of the two curves can

subsequently be compared by using a two-tailed t-test at

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a predefined significance level (50). However, a p-value

does not provide any absolute numerical value that

characterizes the matrix effect. For this reason, it seems

more useful to calculate the matrix effect in the same way

as in the post-extraction method, namely by calculating the

percent ratio of the slopes of the standard addition curve

and the standard curve in neat solution (4,16,49,51,52).

Limit of Quantification: In accordance with EMA and

FDA guidelines on bioanalytical method validation, the

limit of quantification (LOQ) is defined as “the lowest

concentration of analyte in the sample which can be

quantified reliably, with an acceptable accuracy and

precision” (6,8). Acceptable refers to an accuracy value

of 20% from the nominal concentration, and a precision

value of less than 20%. Both guidelines further restrict

the definition of LOQ as the lowest concentration level

of the calibration curve that was created in authentic

matrix. Another common approach to determine

the LOQ is the determination of the concentration

corresponding to a signal-to-noise ratio of 10 (53).

Both definitions impose some issues when the

surrogate matrix approach is used. The EMA and

FDA expect that the LOQ is evaluated in authentic

matrix. When utilizing the surrogate analyte approach,

the surrogate analyte can be used to determine the

LOQ (30). Although the ICH draft guideline does not

encompass any guidance concerning the determination

of the LOQ when dealing with endogenous compounds,

the standard addition method and the surrogate

matrix approach demand an alternative approach.

In this context, it is interesting to discriminate between

the instrumental LOQ (iLOQ) and the method LOQ (mLOQ)

(54). While the iLOQ is a measure to characterize the

performance of an instrument itself, the mLOQ considers

the sensitivity of the actual method in the sample. The latter

thereby considers potential loss in response as a result of,

for example, procedural errors or matrix effects. The iLOQ

can be easily determined in solvent. In contrast, the mLOQ

is not as easily transferable to endogenously present

molecules when SAM or the surrogate matrix approach is

employed. There might be, for example, pronounced ion

suppression present in the matrix, and as a result, the LOQ

determined in solvent will differ from the LOQ in matrix.

For this reason, Tsikas suggested to define the LOQ as

“a representation of the lowest added analyte concentration

(CLOW+

), which, upon addition to the biological sample, can

be experimentally measured with acceptable accuracy

(i.e. max. ± 20% deviation of the nominal value) and

precision (max. RSD 20%)” (46). In the same way as for

accuracy, the CM and C

0, representing the concentrations

upon spiking and the basal concentration, respectively, are

determined by using either SAM or the surrogate matrix

approach. The accuracy is calculated in accordance

with the following formula, in which CLOW+

represents the

lowest concentration of the spiked analyte that generates

an accuracy value that falls within the limits (equation 9):

Accuracy (%) = 100%

C

xC

C–M

LOW+

0

[9]

Conclusion

The quantification of endogenous compounds imposes a

challenging task for the analyst because of the absence

of a true blank matrix, which is required by FDA and EMA

in the preparation of calibrators. Particularly in LC–MS,

it is important to consider the influence of the matrix on

the quantification as a result of matrix effects. Moreover,

the current description of the validation parameters

provided by the regulatory agencies provides a unique

focus on the quantification of exogenous compounds and

it should be appreciated that not all of them are directly

transferable to the context of endogenous compounds.

Very recently, the ICH has issued a new provisional

guideline that contains guidance on the validation of

methods used to quantify endogenous components (9).

A few ways are used to bridge the difficulties in the

quantification process. Among them, the surrogate matrix

approach offers the most straightforward way provided

that an IS is available. Nonetheless, the mere availability

of an IS does not guarantee instant success for accurate

quantification, for example, in case of differences in

elution time between the IS and the natural analyte. Its

validity should therefore be thoughtfully addressed, not

only in terms of coelution, but also in terms of mutual

suppression. The surrogate analyte approach, on the

other hand, offers the option to set the LOQ in the

actual matrix without additional spiking and to prepare

QC samples below the endogenous concentration

levels, but its use might be limited due to the need

for two ISs. In addition, in multicomponent analysis,

utilizing an IS for each compound of interest might be

impeded because of commercial unavailability. In the

latter case, SAM might provide a viable alternative.

Regarding method validation, the use of the surrogate

matrix or the surrogate analyte should be justified by

proving parallelism between the surrogate matrix and the

authentic matrix, or between the surrogate analyte and

the authentic analyte, respectively. For this purpose, the

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comparison of slopes can be used as an alternative for

the determination of accuracy at different concentration

levels. As a result of the unavailability of a true blank

matrix, the assessment of accuracy can be determined

by comparing the difference between the concentration

found after spiking and the endogenous concentration

with the nominal spiked concentration. It is clear that

in this way, accuracy cannot be determined below the

endogenous concentration in the QC sample. In contrast,

the surrogate analyte approach offers the advantage of

evaluating accuracy below the endogenous concentration

of the natural analyte. In the same way, the LOQ can

be determined by simple use of the surrogate analyte

rather than, as is the case for the other approaches,

defining the lowest concentration that can be spiked to

generate an accuracy value within predefined limits.

Coping with the unavailability of a blank matrix in this

particular context might seem challenging at first sight.

However, even without the use of an IS, quantification

of endogenous concentration levels can still be

achieved through the standard addition method. Of

course, developing an adequate validation strategy is

key in the generation of reliable results. The constant

growth of the realm of metabolomics and biomarker

research has prompted the regulatory agencies to

provide a homogenous validation strategy regarding

the quantification of endogenous compounds.

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Maxim Nelis is a Ph.D. student at the University

of Leuven (KU Leuven) in Belgium. His current

research focuses on the identification and

quantification of small molecules in biological

specimens collected from IBS patients with

the objective to find a biomarker.

Patrick Augustijns is a professor in biopharmaceutics

at KU Leuven. His laboratory has developed

a unique technique to collect gastro-intestinal

samples. Upon quantification of drugs and

metabolites in these samples, this approach

allows the gastro-intestinal behaviour of drugs and

formulations to be linked to the systemic outcome.

Deirdre Cabooter is the editor of “Pharmaceutical

Perspectives”. She is a research professor at the

Department of Pharmaceutical and Pharmacological

Sciences of KU Leuven. Her research interests include

studying mass transfer in liquid chromatography,

analyzing complex samples in diverse fields of

application, retention modelling, and solutions for

automated method development. She is also a member

of LCGC Europe’s editorial advisory board. Direct

correspondence about this column to the editor-in-chief,

Alasdair Matheson, at [email protected]

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Mobile Phase Buffers in LC:Effect of Buffer Preparation Method on Retention RepeatabilityDwight R. Stoll1 and Devin M. Makey2, 1LC Troubleshooting Editor, 2Gustavus Adolphus College, St. Peter, Minnesota, USA

For liquid chromatography (LC) methods where the buffer pH and composition have an influence on retention,

which buffer preparation method will provide the most repeatable results?

The measurement of pH, one of the most

common of all analytical measurements,

plays a major role in many chemical

processes, affecting everything from

the productivity of bioreactors in the

biopharmaceutical industry, to the

performance of separation methods

in liquid chromatography (LC) and

electrophoresis. Given that pH

measurement is so common, I think

we can be lulled into the perception

that it is also simple, and that the pH

reported by any benchtop pH meter

can be accepted at face value under all

circumstances. In my interactions working

with people at a variety of experience

levels over the years, I have often felt that

people preparing buffers for use in LC

are a little too trusting of the pH values

reported by pH meters under ordinary

circumstances. In preparation for this

month’s “LC Troubleshooting” column, my

student Devin Makey and I performed

some experiments to see if we could

move in the direction of getting answers

to questions around the topic of the “best”

way to prepare buffers for use in LC. What

follows here is a description of those

experiments, and the data we observed.

I believe that the results are interesting,

and can support best practices for

improving the reliability of LC methods.

I know they are certainly affecting the

way we operate in my laboratory, and I

hope you will find them useful as well.

Dwight Stoll

Introduction

The Role of Eluent pH in LC: The pH

of the eluent has a significant impact

on retention and peak shape in several

modes of LC separations. This is

well understood in reversed-phase

separations, where retention is strongly

dependent on the solubility of the analyte

in the organic-aqueous eluent. The pH

of the eluent affects the charge state

of various functional groups (COOH,

NH2, and so forth), and the charge

state of these functional groups has

a major impact on the solubility of the

analyte in water; this is the origin of the

primary influence of pH on retention. For

example, a simple weak organic acid like

benzoic acid will be neutral (uncharged)

in eluents buffered well below the pKa

(~4.1), because the carboxylic acid

functional group will be protonated.

However, in eluents buffered well above

the pKa, the carboxylic acid functional

group will be deprotonated, and carry a

negative charge. The strong interactions

between the negatively charged

carboxylate group and the highly dipolar

water molecules result in a much higher

water solubility of the benzoic acid

in the high pH eluent, and thus lower

reversed-phase retention under these

conditions. This is exemplified by the

experimental retention data shown in

Figure 1 for benzoic acid on a C18

reversed-phase column, where the

eluent was buffered at different pH levels.

The same chemistry is relevant

in hydrophilic interaction

(HILIC) separations, though the

dependence of retention on pH

is often more complicated than it

is in reversed-phase separations

because of the more influential role

of electrostatic interactions between

the analyte and the stationary phase

in HILIC. The influence of pH on other

LC modes, such as ion-exchange,

is even more evident because the

magnitude of electrostatic interactions

between the analyte and stationary

phase is the dominant factor

influencing retention. Thinking through

these examples, it is clear that pH

adjustment of buffered eluents is a

topic with broad implications in LC.

Current Perspectives on Buffer

Preparation: We also recognize that

buffer preparation and pH adjustment

is a pretty controversial topic in the LC

community. This topic has been covered

on multiple occasions in this column,

focusing on aspects including buffer

selection (1), preparation methods (2,3),

and the idea of solution pH when an

organic solvent is added to the mix (4). In

a recent article of our own, we discussed

the effects of different methods of

buffer preparation on results from HILIC

separations (5). In our preparation for

this instalment, we have found, through

discussions with a variety of people, that

they often have strongly held beliefs

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about what is right and wrong when it

comes to buffer preparation, but also

that these positions are not always

clearly supported by experimental

evidence. With this as a backdrop,

we set out to make some of our own

measurements with the hope that they

would add to understanding in this area.

The most commonly used approach to

buffer preparation for use in LC involves

adding a salt of a buffering agent to

water, then adding a small volume of

relatively concentrated acid or base

solution until a target pH is reached

(as indicated by a pH electrode), and

finally diluting to a specified volume. For

example, suppose we are interested

in making 1 L of phosphate buffer at

pH 6. Although there are many ways to

prepare this buffer, a commonly used

approach would be to first add sodium

hydrogen phosphate (Na2HPO

4) to

about 900 mL of water. The pH of this

initial solution will be about 9. Then, we

could add phosphoric or hydrochloric

acid to the solution slowly and watch

the pH meter, stopping the addition of

acid when the meter reads 6.00. We

could then transfer the solution to a 1 L

volumetric flask, and fill it to the mark

with water. The focus of this article is

really trying to answer the question, “If

we make this buffer ten times, will we

have added exactly the same amount

of acid when we have stopped at pH

6.00, according to the pH meter?” If the

answer is “yes”, then all is well, and we

should expect similar results from LC

separations involving these ten buffers.

We will show that more often than not

the answer is “no”, and that the extent

of variation of the acid added from one

buffer to the next is enough to cause

measurable variability in retention in

some cases. At this point you may be

asking yourself, “How can the answer

possibly be ‘no’?” That in itself is a

good question, and one that requires

many more words than we can fit in this

short article. We’ll come back to this

question at the end of our discussion,

and suggest some reading material

for those interested in really digging

into this more. For now, on to the data.

Experiments, Results, and

Discussion

Dependence of Retention on pH for

Some Probe Molecules: As a first

step in this work, we set out to identify

some simple probe molecules to use

under reversed-phase conditions, and

measure the dependence of their

retentions on eluent pH. We chose one

neutral molecule (ethylbenzene), one

weak acid (butylbenzoic acid, pKa ~4.2),

and two weak bases (4-hexylaniline,

pKa ~4.8; and 4-aminobiphenyl, pK

a

~4.3), and used uracil in our test mixture

as a column dead time marker. We

then prepared about 500 mL each of

nine potassium phosphate buffers with

expected aqueous pH values between

2.80 and 3.20, in increments of 0.05

units. The approach was to first add

potassium phosphate (the same amount

in each case, 30 millimoles), then add

different amounts of phosphoric acid

as needed to reach the target solution

pH, and finally add enough water to

reach a total mass of 500.0 g. These

amounts are shown in Table 1, and

were calculated by solving the charge

balance equation for this system for the

number of moles of phosphoric acid that

was required at each pH level. Activity

coefficients were calculated using the

extended Debye-Hückel equation (6).

Using each of these buffers as the

aqueous component of the eluent, we

measured the retention times of the four

probe compounds on a C18 column.

The resulting chromatograms for five of

the buffers are shown in Figure 2, and

a plot of the retention factors of the

three ionizable probes relative to the

retention factor of ethylbenzene is shown

in Figure 3. At this point we make two

observations. First, Figure 2 shows that

the retention of ethylbenzene is nominally

independent of pH, as expected, allowing

us to normalize the retention of the

other three probe compounds to the

retention of ethylbenzene to minimize

20

15

10

5

0

4 5 6 7 8

Eluent pH (Aqueous Phase)

Rete

nti

on

Fact

or

3

1600

1

2

34 5

1200

800

400

Time (min)

pH = 3.15

pH = 3.05

Sig

na

l (m

AU

, 2

54

nm

)

pH = 2.95

pH = 2.85

0

0 1 2 3 4 5

FIGURE 1: Effect of eluent pH on the

retention of benzoic acid under

reversed-phase conditions.

Chromatographic conditions: column,

SB-C18; eluent, 10:90 acetonitrile–

phosphate buffer; temperature, 40 °C.

FIGURE 2: Effect of eluent pH on the

retention of probe compounds (2)

4-aminobiphenyl, (3) n-butylbenzoic

acid, (4) 4-hexylaniline, and (5)

ethylbenzene. Uracil (1) was used as

a dead time marker. Chromatographic

conditions: column, StableBond C18

(50 mm × 4.6 mm, 3.5-μm); flow rate,

2.0 mL/min.; eluent, 40:60 acetonitrile–

buffer; temperature, 40 °C.

366 LCGC Europe July 2019

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the effects of other variables such as

temperature and organic to water ratio

in the eluent on these measurements.

On the other hand, the retention of the

other three probes all exhibit some

dependence of retention on pH, with the

hexylaniline being the most sensitive

of the three by far. Second, Figure 3

shows that the observed retention of

each of the three ionizable probes is

a smooth function of the calculated

pH. Although the exact dependence

of retention on pH is unknown for

these conditions, we would at least

expect it to be a smooth relationship.

Comparison of pH Meter-Directed

and Gravimetric Methods of Buffer

Preparation: Now, let’s return to our

1.0

0.8

0.6

k/k

eth

ylb

en

ze

ne

0.4

0.2

0.0

2.8 3.0 3.1 3.2

pH

2.9

FIGURE 3: Retention of the three

ionizable probes relative to the

retention of ethylbenzene. Conditions

are as in Figure 2. Key: O hexylaniline,

O butylbenzoic acid, O aminobiphenyl.

TABLE 1: Reagents added to make 0.5 L potassium phosphate buffers solutions in the

range of pH 2.8 to 3.2a.

Mass

KH2PO

4 (g)

Mass 85% H3PO

4(g) Expected PH Measured pH

4.083 0.75 2.80 2.84

4.083 0.67 2.85 2.84

4.083 0.60 2.90 2.92

4.083 0.54 2.95 2.97

4.083 0.47 3.00 2.94

4.083 0.43 3.05 3.04

4.083 0.37 3.10 3.12

4.083 0.33 3.15 3.17

4.083 0.30 3.20 3.12

aThe pHs of all solutions used in this work were measured using a low sodium error glass

electrode (Orion 8101BNWP ROSS Half-Cell Electrode, from Thermo Scientific (Waltham, MA,

USA), calibrated using pH 1.68 and 4.00 standards from VWR (West Chester, PA, USA).

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question above: “If we make this buffer

ten times, will we have added exactly

the same amount of acid when we have

stopped at pH 6.00, according to the pH

meter?” We prepared three replicates of

a nominal pH 3 buffer as described in

Table 1 by using two different methods:

A) pH meter-directed: In this case,

we use the pH meter to decide when

to stop adding phosphoric acid (for

example, when the meter reads 3.00).

B) Gravimetric: In this case, we

calculate the amounts of each reagent

ahead of time, and repeat that recipe

each time, only measuring the pH of the

solution when the buffer is complete.

The nominal procedures for the

two methods, and the amounts of

reagents added for the six buffers

used to obtain the data shown in

Figure 4, are shown in Table 2.

Figure 4 shows the mean relative

retention of hexylaniline measured for six

different buffers prepared by the same

analyst, three by the pH meter-directed

method (all using the same meter and

electrode), and three by the gravimetric

method. The results are quite clear. They

show that the buffers prepared using

the gravimetric method lead to much

better repeatability of retention time in

different buffers, relative to the repeatability

observed for different buffers made

using the pH meter-directed approach.

These results are evidence that the

answer to our question posed earlier in

this article is “no”. In other words, the

pH values reported by the meter are not

sufficiently repeatable to guide preparation

of the buffer when buffers of highly

repeatable composition are needed.

Having settled on the protocol shown in

Table 2 for the gravimetric method, three

other analysts from our laboratory each

prepared three replicate buffers using

the pH meter-directed approach, and

three using the gravimetric approach.

The results are shown in Table 3, where

we see that all four analysts were

able to produce buffers that led to

highly repeatable retention time using

the gravimetric approach, whereas

the buffers prepared using the pH

meter-directed approach always led to

much more variable retention times.

Closing Thoughts

Clearly not all work involving buffered

solutions requires the level of repeatability

in pH that we explored in this work.

However, we believe these results show

that, when working with analytes that

0.680 (a) (b)

kh

ex

yla

nil

ine/k

eth

ylb

en

ze

ne

kh

ex

yla

nil

ine/k

eth

ylb

en

ze

ne

0.695

0.690

0.685

0.680

0.6751 2 31 2 3

0.675

0.670

0.665

0.660

Buffer# Buffer#

FIGURE 4: Relative retention of hexylaniline (normalized to ethylbenzene) for six

buffers prepared by the same analyst; (a) for pH meter-directed approach, and (b) for

gravimetric approach. Chromatographic conditions are as in Figure 2. Details of the

buffer preparations are given in Table 2. Error bars represent one standard deviation

for ten replicate injections of the probe compound with a given buffer.

TABLE 2: Buffer preparation steps and amounts of reagents added for three different

replicate buffers made using the pH meter-directed and gravimetric approaches.

Buffer Number

Step pH Meter-Directed Approach 1 2 3

1 Weighed 4.0827 g KH2PO

4 in a weighing boat 4.0827 g 4.0827 g 4.0827 g

2 Transferred salt to 500 mL beaker

3 Rinsed weighing vessel 4× with H2O

4 Added 450 g H2O

5 Titrated to pH 3.00 with 0.85% H3PO

429.3 mL 26.9 mL 24.9 mL

6Transferred solution to 500 mL volumetric

flask and filled to line with H2O

Buffer Number

Step Gravimetric Approach 1 2 3

1Weighed 4.0827 g KH

2PO

4 in a weighing

boat4.0827 g 4.0828 g 4.0827 g

2 Weighed 28.179 g 0.85% H3PO

4in a beaker 28.1727 g 28.1788 g 28.1734 g

3 Transferred salt and acid to solvent bottle

4 Rinsed weighing vessels 4× with H2O

5 Diluted up to 500 g with H2O 500.03 g 500.02 g 500.00 g

Measured pH 2.98 2.97 2.96

TABLE 3: Percent relative standard

deviation (% RSD) of relative retention of

hexylaniline measured using buffers (n(( = 3

in each case) prepared by four different

analysts and two different methods.

Analyst

Approach

pH Meter-

DirectedGravimetric

1 2.72 0.06

2 2.23 0.10

3 2.34 0.02

4 1.25 0.003

368 LCGC Europe July 2019

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have a significant retention dependence

on pH of the eluent, the gravimetric

approach to buffer preparation is worth

considering seriously. Simply put, in most

cases weighing reagents using a balance

is a simpler operation than measuring pH

using a glass electrode, and can be done

with extraordinary precision compared

to most other analytical methods. When

the recipe for a particular buffer is

known, and repeating the preparation of

the buffer in a precise way is desirable,

then the gravimetric approach is most

precise. Readers interested in learning

more about factors that influence

the accuracy and precision of pH

measurement at this level are referred

to Bates’ book on the topic (7). Finally,

readers interested in tools for calculation

of buffer recipes that can be used with

a gravimetric approach are referred to

free web-based tools developed by

Professor Rob Beynon (https://www.

liverpool.ac.uk/pfg/Research/Tools/

BuffferCalc/Buffer.html), and Professor

Peter Carr and Aosheng Wang (http://

zirchrom.com/Buffer.asp) It is important

to recognize that the latter tool does not

correct pH calculations to account for

activity effects, which affect calculated

pHs of solutions of high ionic strength

and multiply charged buffer components

(for example, phosphate at pH 7).

Acknowledgements

We’d like to acknowledge the effort of

Hayley Lhotka, Alex Florea, and Gabriel

Leme and their willingness to participate

in the experiments described here. We

also thank Professor Peter Carr and Dr.

William Tindall for their willingness to share

their knowledge of this subject with us.

DM was supported by a grant from the

Camille and Henry Dreyfus Foundation.

References1) G.W. Tindall, LCGC North Am. 20, 1114–1118

(2002).

2) J.W. Dolan, LCGC Europe 28(1), 40–44 (2015).

3) G.W. Tindall, LCGC North Am. 21, 28–32 (2003).

4) G.W. Tindall, LCGC North Am. 20, 1028–1032

(2002).

5) D.R. Stoll and C. Seidl, LCGC Europe 31(3),

144–148 (2018).

6) L.W. Potts, Quantitative Analysis: Theory and

Practice (Harper & Row, New York, New York,

USA, 1987).

7) R.G. Bates, Determination of pH: theory and

Practice (John Wiley and Sons, New York, New

York, USA, 2nd ed.,1973).

Dwight R. Stoll is the editor of “LC

Troubleshooting” and professor and

co-chair at Gustavus Adolphus College.

Devin Makey is an undergraduate

student in his fourth year of

study in chemistry at Gustavus

Adolphus College.

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Temperature Programmed GC: Why Are All Those Peaks So Sharp?Nicholas H. Snow, Department of Chemistry and Biochemistry, Seton Hall University, New Jersey, USA

Temperature programming is used for most separations in capillary gas chromatography (GC) today. Despite

this, many of the principles by which we understand temperature-programmed capillary column separations

are based on ideas developed using packed columns and isothermal conditions. This instalment of “GC

Connections” dives into temperature programming. First, the differences in peak widths and retention times

between temperature programmed and isothermal chromatograms are examined. Why are all the peaks so

sharp in temperature programmed GC, yet they get broader (and shorter) in isothermal GC? Next, we explore

some early ideas about temperature programming and peak broadening that explain why the peaks are so

sharp in temperature-programmed GC, and why the peak spacing is different from isothermal GC. Finally,

we examine an important consequence of our ability to program temperature: the need for temperature

programming in splitless and other injections that use “solvent effects” and other peak focusing mechanisms.

These points are illustrated using several historical figures and chromatograms from the early days of GC.

Nearly every student of gas

chromatography (GC) has seen

chromatograms like the ones shown in

Figure 1. These chromatograms were

originally published in 1959, in one of

the first papers describing an apparatus

for temperature programming (1).

Although developed on a handmade

packed column with firebrick as the

stationary phase, this work shows the

same comparison and contrast between

isothermal and temperature-programmed

GC seen today. Starting from the

bottom, Figure 1(c) shows an isothermal

separation of normal alkanes. Notice

that as the retention times get longer, the

peaks get broader, and the last peak

appears to exhibit fronting. Also notice

that the retention time difference between

each peak appears to nearly double with

each successive alkane. The difference

between C9 and C10 (the last two peaks)

is about twice the difference between C8

and C9. Notice also that nearly 30 min

is required to separate the six alkanes.

This chromatogram illustrates the main

limitations of isothermal GC. First, the

range of analytes that can be separated

in a reasonable time is relatively small.

Second, as the retention times get

longer, the peaks get significantly

broader (band broadening), and, as a

result, they get shorter and harder to

detect. If the peak area is constant, as a

peak becomes broader, it must become

shorter, limiting sensitivity. Third, the

fronting of the later peaks is caused by

the column temperature being too low

for effective adsorption on the surface of

the stationary phase. The liquid analyte

condenses on the surface, causing some

to be evaporated into the mobile phase

more quickly and to therefore elute too

soon. This is a form of column overload.

Moving up, Figure 1(b) shows a

temperature-programmed separation

of the same mixture of n-alkanes with a

temperature programming rate of 5 °C

per min and Figure 1(a) shows the same

separation with a rate of 30 °C per min.

Note the significant differences from

the isothermal separation. First, the run

time is reduced from 30 min to 10 and

5 min, respectively. Second, the peaks

are spaced evenly. The retention time

difference between each successive

alkane is about the same. Finally, all of

the peaks are sharper (remember this

was a handmade packed column); they

appear to have about the same peak

width and as a result all have about the

same peak height, while the isothermal

peaks get broader and shorter.

Figure 1 raises two critical questions:

1. Why are the retention times

evenly spaced in the temperature

programmed separation, while

the spacing doubles from peak

to peak in the isothermal run?

2. Why are all the peaks sharp in the

temperature-programmed separation,

while the later peaks get significantly

broader in the isothermal separation?

We will address these questions by

drawing some simple pictures of the

chromatographic process, followed

by descriptions based on theories

for both isothermal and temperature-

programmed GC that were developed

in the first 10 years of GC.

For an analyte to move along a GC

column, it must have a vapour pressure

of at least a few torr at the operating

temperature. Remember that this

vapour pressure is affected by both

the normal vapour pressure and any

change resulting from interactions with

370 LCGC Europe July 2019

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the stationary phase. Figure 2 shows

a simplified picture of the inside of

a capillary column, with the analyte

molecules represented as dots (2). This

compound has nine dots in the stationary

phase and three in the mobile phase,

giving a retention factor (k) of 3. A higher

value of k indicates that more of the dots,

a larger mass of the analyte, will be in

the stationary phase, causing the analyte

to be retained longer. The carrier gas

forces the three dots in the mobile phase

to move along the column. When they

encounter fresh stationary phase, their

attraction to the stationary phase and

low (but finite) vapour pressure cause

them to condense onto and dissolve in

this new region of stationary phase. In

isothermal GC, the thermodynamics of

the partitioning process between the

mobile phase and the stationary phase is

governed by the enthalpy of vaporization

(the change in heat content) for the

analyte from the stationary phase into

the mobile phase. For the alkanes seen

in Figure 1, the enthalpy of vaporization

increases linearly as each -CH2- unit is

added to the carbon chain. Through the

Gibbs equation, which relates enthalpy

and temperature, this results in an

exponential increase in K and k, leading

to an exponential increase in retention

time. The full theory and thermodynamics

are discussed elsewhere in more detail

with the relevant equations (3–5).

In temperature programming, the

column temperature usually increases

linearly with time as the separation

proceeds. This has the effect of

increasing the vapour pressure and

decreasing k of the analytes with

time. From general and physical

chemistry courses, we know that vapour

pressure increases exponentially

with temperature, with the linearized

form of the relationship expressed by

the Clausius-Clapeyron equation:

[1]

where Pvap

is the vapour pressure, ΔHvap

is the enthalpy of vaporization, R is

the gas constant, T is the temperature

in degrees Kelvin, and β is ΔS/R. Gas

chromatographers often use a similar

expression, the van’t Hoff equation,

which relates the equilibrium constant

for a reaction and the temperature,

assuming a constant change in

enthalpy ΔH, and entropy ΔS:

In K =–∆H

R+ ( )

∆S

R

1

T [2]

where K is the partition coefficient,

which in GC is related to the retention

factor (k) by the phase ratio (β), the ratio

of the volume of the stationary phase

to the volume of the mobile phase. In

1963, less than 10 years after the initial

inception of GC, Giddings provided a

model for temperature programming,

depicted in Figure 3, based on the

Clausius-Clapeyron equation, modified

for the specific case of GC and on

relationships derived previously by Dal

Nogare and Harris and Habgood (6–9).

One equation for describing temperature

programming and relating it to the same

(a)

0

0

0

2

21

3

3

6

4

8

8 16 24 32

2 MV.

4 MV.

5

10DETEC

TO

RR

ESPO

NSE

(b)

(c)

FIGURE 1: Temperature-programmed and isothermal chromatograms of a C5–C

10 alkane

mixture. The temperature program in (a) is 30 °C per minute starting at 40 °C and in (b) is

5 °C per minute starting at 40 °C, and (c) is isothermal at 75 °C. Reproduced with

permission from reference 1, American Chemical Society (copyright 1959).

FIGURE 2: Simplified picture of analyte partitioning in a capillary GC column. Analyte

molecules are represented by dots. There are nine dots in the stationary phase and

three in the mobile phase, giving k = 3. Reprinted from reference 2 with permission of

the author.

372 LCGC Europe July 2019

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thermodynamic quantities as seen in

isothermal GC and derived by Harris

and Habgood is seen in equation 3.

T

∫ αe

β

R dTRate=

To tM(T) 1+ ( ( ) )∆H/RT

[3]

where To is the initial temperature

of the temperature program, TR is the

elution temperature of the analyte, tM(T)

is the gas hold-up time at temperature

T, α = ΔS/R, and β is the column phase

ratio. Rate is the slope (°C/min) of the

linear temperature program. Equation 3

must be solved numerically for the

second integration constant, which

provides the elution temperature of the

analyte (easily translated into retention

time using the starting temperature

and programming rate), and provides

the basis for several of the computer

simulation programs for GC that have

been developed over the years (10,11).

For computer simulations of GC, ΔH

and ΔS are easily measured and

have been termed thermodynamic

retention indices (12). With knowledge

of these for a given analyte and

stationary phase, and equation 3, it is

possible to predict the retention time

of any analyte on that same stationary

phase under any conditions.

In Figure 3, the exponential curve

describes the rate of zone or peak

migration as the column temperature

in increased. This exponential curve

resembles a vapour pressure curve, and

can be approximated as such, with the

addition that acceleration of the analyte

along the column is faster than predicted

by vapour pressure alone, due to

expansion of the carrier gas as it travels

from the higher pressure at the column

inlet to the lower pressure at the outlet.

This demonstrates that, as the column

temperature is increased, the peak

accelerates as it simultaneously travels

along the column because its vapour

pressure increases and the carrier

gas is expanding inside the column

as it flows from the inlet to the outlet.

In order to simplify the model, the

exponential curve is broken up into

six 30 °C steps, a so-called “step

approximation” for temperature

programming. As seen in Figure 3,

with temperature programming

conditions, in contrast to isothermal

conditions, analytes move slowly

when first injected, and accelerate

exponentially as the temperature is

increased and the chromatographic

run proceeds. This exponential

acceleration has the practical effect

of linearizing the relationship between

carbon chain length and retention time

for the n-alkanes, as seen in Figure 1.

As an example of using the step

approximation, Giddings described a

temperature program from 85 to 265 °C,

with the steps being six 30 °C intervals.

He demonstrated that 50% of a peak’s

migration down the column occurs in the

final 30-degree segment. In short, the

peak travels about half of the column

length in the last 1/6 of the retention

time, and about 3/4 of the column length

0.15

0.10

ACTUAL

INCREASE

STEP FUNCTION

ELUTIONTEMPERATURE

T

APPROXIMATION

0.05

0100 130 160 190 220 250 265

RELA

TIV

E M

IGR

ATIO

N R

ATE

85

FIGURE 3: Step function

approximation for the rate of zone

migration in temperature-programmed

gas chromatography. Reprinted with

permission from reference 6, American

Chemical Society (copyright 1962).

LOWER DETECTION LIMIT

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in the last 1/3 of the total retention time.

Likewise, at the beginning of the run, the

peak travels about 1/64 of the column

length in the first 1/6 of the retention time,

and about 3/32 of the column length

in the first 1/3 of the retention time.

From this discussion, we

see that retention times in

temperature-programmed GC are

based on the same thermodynamic

quantities as in isothermal GC. However,

in temperature programming, in

contrast to isothermal conditions, the

relationship between the enthalpy of

vaporization and the retention time

becomes linear, due to the linear

increase in temperature giving rise to an

exponential increase in vapour pressure,

as seen in the Clausius-Clapeyron

equation, or in K as seen in the van’t

Hoff equation. This explains the first

aspect of the temperature programmed

chromatogram seen in Figure 1:

alkane peaks are evenly spaced.

Turning to the second observation

about Figure 1, that all of the peaks in

the temperature-programmed run are

of similar width, the step approximation

can help explain that, as well. Giddings

developed the step approximation so

that the six segments could be further

approximated as isothermal segments

at the mean temperature of the segment.

This allows us to think about each

segment as a single isothermal portion

of the run, and to apply the Golay

equation, shown below in abbreviated

form, to the conditions in each segment:

H =B +(C

s + C

M)

uu [4]

where H is the height equivalent to a

theoretical plate, B is related to solute

diffusion rates in the mobile phase, CS

and CM are related to mass transfer rates

in the stationary and mobile phases,

respectively, and � is the average velocity

of the carrier gas. A full explanation of

the Golay equation and the principles

related to the kinetics of band

broadening is provided in references

4 and 5. The Golay equation reminds

us that the rate of band broadening

(expressed by H, the height equivalent

to a theoretical plate) is a consequence

of diffusion in the mobile phase, mass

transfer in the mobile phase, and mass

transfer in the stationary phase, as well.

Simplified views of diffusion and mass

transfer are shown below in Figure 4.

From the Golay equation, we see that

band broadening caused by diffusion

in the mobile phase, illustrated in

Figure 4(a), is inversely related to the

average linear carrier gas velocity. Using

the step model, we see that, in the first

segments immediately following the

injection, the bulk of analyte molecules

reside in the stationary phase, so they

are not affected much by mobile phase

diffusion. As the separation proceeds in

the later segments, the bulk of analyte

molecules are in the mobile phase, and

move very rapidly as they approach

the column outlet. This minimizes band

broadening due to molecular diffusion

because of the inverse relationship

with the carrier gas velocity.

Next, we turn to band broadening

due to mass transfer, which is somewhat

more complicated, but can be explained

using similar logic. In capillary columns,

there are terms related to mass transfer

in both the mobile and stationary

phases. In this case, the rate of band

broadening is directly proportional to the

average velocity of the carrier gas, and

is related to k and the respective mobile

phase and stationary phase diffusion

constants, illustrated in Figure 4(b). On

(a)

Flow

Mobile

Phase

Stationary

Phase

(b)

FIGURE 4: Diffusion and mass transfer in a capillary column: (a) molecular diffusion

occurring in the mobile phase and relating to the B term in the Golay equation; (b)

mass transfer occurring in both the mobile and stationary phases and referring to the

C terms in the Golay equation.

374 LCGC Europe July 2019

GC CONNECTIONS

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the left side of the figure, a symmetrical

peak with k = 3 is shown, with its relative

portions in both phases. On the right

side of Figure 4(b), the peak is seen to

distort, or spread, caused by the mass

in the mobile phase being shifted down

the column (to the right in the figure),

followed by the resulting evaporation

of new analyte on the left of the figure.

The step approximation is useful

here, as well. In the early steps, with

the bulk of analyte molecules in the

stationary phase, mass transfer is limited

by the low temperature at the start of

the temperature program. The analyte

band is essentially “frozen” in place. In

later segments, when the bulk of the

analyte molecules are in the mobile

phase, the time spent to traverse 50%

of the column is short—1/6 of the total

retention time—limiting the effect of mass

transfer in the mobile phase. For mass

transfer in the stationary phase, k gets

smaller as the temperature increases,

pushing the analyte more and more out

of the stationary phase into the mobile

phase, also limiting stationary phase

mass transfer. In short, the narrow initial

band, once it starts to move, accelerates

and moves very quickly along most

of the column length, minimizing the

time for significant mass transfer as it is

moving. The Golay equation and the step

approximation together explain why the

peaks are all sharp and about the same

width in temperature-programmed GC.

The step approximation also provides

a useful explanation for many practical

aspects of temperature-programmed

GC beyond the appearance of the

chromatogram in Figure 1. Best practice

in performing splitless injections provides

a good example. The basics of splitless

injection were recently reviewed in

this column, and are the subject of an

excellent review and book by Konrad

Grob, so they will not be reviewed

again in detail here (13–15). For this

discussion, the important principles in

splitless injections are that the injection

process itself may require up to 60 s

to complete, and splitless injection

is always used in combination with

temperature programming. Despite

the long time required for the injection

process, the peaks seen in separations

that employ splitless injection are

often very sharp. The step model

of temperature programming can

help to explain this phenomenon.

In a splitless injection, there are

two peak focusing mechanisms at

work once the sample reaches the

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column: solvent effects, and thermal

focusing or “cold trapping”. The step

approximation explains how both can

work in combination with temperature

programming to generate sharp peaks.

First, assume a splitless injection

in combination with a temperature

program that starts at a temperature

well below the boiling point of the

sample solvent, and even further below

the boiling points of the analytes. For

example, if using hexane as solvent,

which has a normal boiling point of

68 °C, I start my temperature programs

at 40 °C. As the sample and solvent

transfer into the column, the low

initial column temperature causes the

solvent to condense as a long plug

of liquid at the head of the column.

Analytes with higher boiling points

or strong affinity for the stationary

phase will be strongly retained by the

stationary phase. This is cold trapping.

Analytes with lower boiling points or

stronger affinity to the solvent will be

initially retained in the solvent plug,

followed by retention as a narrow

initial band on the stationary phase

as the solvent evaporates. This is the

solvent effect. A detailed description

of solvent effects is provided in the

text and article by Grob (14,15)

The step approximation applies

to splitless injections whether the

peaks are refocused by solvent effects

or by cold trapping. All the peaks are

broadened as the splitless injection

process proceeds during the initial

purge-off time, with the peak width

determined by the length of the

purge-off time. The cold initial column

temperature effectively condenses

the analytes into a narrow band at the

column head. As the column is heated,

the analytes begin to move down the

column one by one, determined by their

heat of vaporization from the stationary

phase to the mobile phase. The

process is similar for solvent effects,

except that the initial bands

are focused by evaporation of

the solvent plug during the early

stages of the separation. As an

example, picture two analytes, one with

a retention time of 12 min, and

one with a retention time of 18 min.

When the first analyte elutes after

12 min, the second analyte will have

travelled about 1/4 of the column

length. It will travel the final 3/4 of the

column in the remaining 6 min. As

discussed above, this process of

refocusing, either by cold trapping or

solvent effects, followed by temperature

programming, keeps all of the peaks

in a splitless injection sharp.

Temperature-programmed GC has

been in common use for about six

decades, and continues to be among

the most powerful, yet easy to use,

high resolution separation methods

available. However, much of the theory

of GC was developed assuming

isothermal conditions, and continues

to be discussed on that basis. The

theory of temperature-programmed

GC is much more complex than for

isothermal GC, but is still based on

the same fundamental thermodynamic

and kinetic principles. In temperature

programmed GC, retention time

relates linearly to the enthalpy of

vaporization, while in isothermal GC the

relationship is exponential. Combined

with the high temperature stability of

columns, this allows a wide range of

analytes to be separated in a single

run. The temperature-program step

approximation provides a simple means

for understanding how the peaks in

temperature programmed GC remain

sharp throughout the run, based on

acceleration of the migration rate along

the column as the temperature program

proceeds. These principles make

temperature-programmed capillary GC

still the most powerful chromatographic

separation technique available today.

References1) S. Dal Nogare and J.C. Harden, Anal. Chem.

31(11), 1829–1832 (1959).

2) N.H. Snow, LCGC Europe 31(11), 616–623 (2018).

3) N.H. Snow, J. Chem. Educ. 73(7), 592–597 (1996).

4) L.M. Blumberg, Gas Chromatography, C.F. Poole,

Ed. (Elsevier, Amsterdam, The Netherlands,

2012), pp. 19–78.

5) H.M. McNair, and J.M. Miller, Basic Gas

Chromatography (John Wiley and Sons, New

York, New York, USA, 2nd ed., 2008), pp. 29–52.

6) J.C. Giddings, J. Chem. Educ. 39, 569–573 (1962).

7) H.W. Habgood and W.E. Harris, Anal. Chem. 32,

450–453 (1960).

8) H.W. Habgood and W.E. Harris, Anal. Chem. 32,

1206 (1960).

9) S. Dal Nogare, Anal. Chem. 35, 19R–25R (1960).

10) N.H. Snow and H.M. McNair, J. Chromatogr. Sci.

30, 271–275 (1992).

11) Pro EZGC Chromatogram Modeler https://www.

restek.com/proezgc (Accessed May 16, 2019).

12) E. Dose, Anal. Chem. 59, 2414–2419 (1987).

13) N.H. Snow, LCGC Europe 31(7), 378–384 (2018).

14) K. Grob, Split and Splitless Injection for Quantitative

Gas Chromatography: Concepts, Processes, Practical

Guidelines, Sources of Error (John Wiley and Sons,

New York, New York, 4th. ed., 2008).

15) K. Grob, Anal. Chem. 66(20) 1009A–1019A (1994).

Nicholas H. Snow is the

Founding Endowed Professor in

the Department of Chemistry and

Biochemistry at Seton Hall University,

and an Adjunct Professor of Medical

Science. He is interested in the

fundamentals and applications of

separation science, especially gas

chromatography, sampling, and

sample preparation for chemical

analysis. His research group is very

active, with ongoing projects using

GC, GC–MS, two-dimensional GC,

and extraction methods including

headspace, liquid–liquid extraction,

and solid-phase microextraction.

“GC Connections” editor John V.

Hinshaw is a Senior Scientist at

Serveron Corporation in Beaverton,

Oregon, USA, and a member of

LCGC’s editorial advisory board.

Direct correspondence about this

column to the author via e-mail:

[email protected]

376 LCGC Europe July 2019

GC CONNECTIONS

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CF200

IS YOUR LAB SOLVENT SAFE?

Report: R1961-01-A | BS EN61010-1 | BS EN61010-2-020

To learn more about our robotic centrifuge

get in touch at [email protected]

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Mass SpectrometerShimadzu’s LCMS-9030 research-grade mass spectrometer is

designed to deliver high-resolution, accurate mass detection

with fast data acquisition rates, allowing scientists to identify and

quantify more compounds with greater confidence, according

to the company. It utilizes the same engineering as Shimadzu’s

rugged, high-performance triple quadrupole (LC–MS/MS)

platform and integrates this with TOF architecture.

www.shimadzu.eu

Shimadzu Europa GmbH, Duisburg, Germany.

HILIC ColumnsHilicon offers a broad range of HILIC products to separate polar

compounds. Three column chemistries in UHPLC and HPLC,

iHILIC-Fusion, iHILIC-Fusion(+), and iHILIC-Fusion(P), provide

customized and complementary selectivity, excellent durability,

and very low column bleeding, according to the company. The

columns are suitable for the analysis of polar compounds in “omics” research,

food and beverage analysis, pharma discovery, and clinical diagnostics.

www.hilicon.com

Hilicon AB, Umeå, Sweden.

(U)HPLC ColumnsYMC-Triart Bio C4 is a wide-pore phase for (U)HPLC

based on the established hybrid-silica particle, YMC-Triart.

As a result of its 300 Å pore size, this column is designed

for peptide, protein, or monoclonal antibody separations.

High temperature (up to 90 °C) and pH (1–10) stability is

provided. Excellent column-to-column, as well as lot-to-lot

reproducibility, is offered, according to the company.

https://ymc.de/rp-bioseparation.html

YMC Europe GmbH, Dinslaken, Germany.

Mass SpectrometerThe Thermo Scientific Orbitrap Exploris 480 benchtop

mass spectrometer combines proven technology,

advanced capabilities, and intelligence-driven data

acquisition strategies for rigorous, high-throughput

protein identification, quantitation, and structural

characterization of biotherapeutics and translational

biomarkers, according to the company.

www.thermofisher.com

Thermo Fisher Scientific, San Jose, California, USA.

Trapping ColumnPharmaFluidics has launched

a μPAC Trapping column with

identical stationary phase

support morphology compared

to the analytical μPAC columns.

By effectively desalting and

preconcentrating the analytes

of interest onto the trap column,

analytical column lifetime and

workflow throughput can be

improved, according to the

company. Dilute samples can be

loaded in a bidirectional way at high

flow rates and with minimal loss of

chromatographic performance.

www.pharmafluidics.com

PharmaFluidics, Ghent, Belgium.

Triple DetectionPostnova has introduced the Triple

Detection for thermal field-flow

fractionation (FFF) and GPC/SEC.

Triple Detection is the combination

of multi-angle light scattering

(MALS), viscosity detection,

refractive index detection, and UV

detection. In a single separation

experiment, Triple Detection

provides molar mass distribution,

molecular size distribution, and

molecular structure (branching,

composition) of polymers,

biopolymers, polysaccharides,

proteins, and antibodies.

www.postnova.com

Postnova Analytics GmbH,

Landberg, Germany.

T r i p l e D e t e c t i o nOnline Coupling to FFF and SEC

FFFSEC

PN3621 MALS Detector

Particle SizeRg / Molar Mass

PN3150 RI Detector

Concentration

PN3310 ViscometerDetector

Intrinsic ViscosityBranching

cosity

+

+

on

e

378 LCGC Europe July 2019

PRODUCTS

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Multi-Angle Static Light ScatteringIntroducing the next generation DAWN

multi-angle static light scattering (MALS)

detector for absolute characterization of the

molar mass and size of macromolecules and

nanoparticles in solution. DAWN offers high

sensitivity, a wide range of molecular weight,

size, and concentration, and a large selection

of configurations and optional modules for enhanced capabilities.

www.wyatt.com/dawn

Wyatt Technology, Goleta, California, USA.

GPC/SEC Validation KitPSS EasyValid is a system suitability test

that evaluates the entire GPC/SEC system.

According to the company, it is ideal for various

aspects of quality assurance qualification,

whether mandated by stringent requirements

(GLP, DIN, ISO 9000× certifications) or good management practices. It

comprises a validation column, calibration standards, and European reference

materials and is available for organic solvents or aqueous systems.

www.pss-polymer.com

PSS GmbH, Mainz, Germany.

Crimping StationThe CR-5000S is a crimping station for 2- to 100-mL vials and

can be used for all types of caps. It is equipped with a rotation

table for a higher rate and screen touch. It is crimping force

adjustable and head height adjustable according to the type

of vial. It is reportedly ideal for pharmaceutical conditioning

and suitable for clean room. According to the company, the

machine is easy to use and has an average rate of 750 vials/h.

www.sertir.fr

Action Europe, Sausheim, France.

Hydrogen GeneratorThe Precision Hydrogen Trace generator supplies GC

carrier gas and GC fuel gas for GC detectors. A safe

alternative to a helium cylinder, this generator offers a

solution for those looking to reduce their reliance on

an increasingly scarce helium supply. According to

the company, the generator can produce up to

1.2 L/min of 99.9999% pure hydrogen.

https://bit.ly/2KY0QgM

Peak Scientific, Scotland, UK

Sample AutomationMarkes’ new Centri

multitechnique platform is an

advance in sample automation

and concentration for

GC–MS, according to the

company, and offers four

sampling modes: HiSorb

high-capacity sorptive extraction,

headspace, SPME, and thermal

desorption. The company

reports analyte focusing allows

increased sensitivity in all

modes, state-of the-art robotics

increases sample throughput,

and sample re-collection allows

repeat analysis without having to

repeat lengthy sample extraction

procedures.

http://chem.markes.

com/Centri

Markes

International Ltd.,

Llantrisant, UK.

Thermal Desorption

SystemThe MPS TD is a dedicated

sampler for automated thermal

desorption, thermal extraction,

and dynamic headspace (DHS)

analysis. MPS TD is compatible

with Gerstel TDU, TD 3.5+,

and DHS processing up to 240

samples. The complete system

including GC–MS is operated with

one integrated method and one

sequence table.

www.gerstel.com

Gerstel GmbH & C0. KG,

Mülheim an de Ruhr, Germany.

379www.chromatographyonline.com

PRODUCTS

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11–13 SEPTEMBER 2019The 12th Balton Symposium on

High-Performance Separation

Methods

Siófok, Hungary

E: [email protected]

W: www.balaton.mett.hu

15–18 SEPTEMBER 2019The 30th International Symposium

on Pharmaceutical and Biomedical

Analysis (PBA 2019)

Tel Aviv, Israel

E: [email protected]

W: www.pba2019.org

29 SEPTEMBER–1 OCTOBER

2019

SFC 2019

Philadelphia, Pennsylvania, USA

E: [email protected]

W: www.greenchemistrygroup.org/

current-conference/sfc-2019

14–16 OCTOBER 2019The 11th Conference of The

World Mycotoxin Forum and the

XVth IUPAC International

Symposium on Mycotoxins

(WMFmeetsIUPAC)

Belfast, Northern Ireland

E: WMF@bastiaanse-communication.

com

W: www.worldmycotoxinforum.org

5–8 NOVEMBER 2019Recent Advances in Food Analysis

(RAFA 2019)

Prague, Czech Republic

E: [email protected]

W: www.rafa2019.eu

29–31 JANUARY 2020The 16th International Symposium

on Hyphenated Techniques in

Chromatography and Separation

Techniques

Ghent, Belgium

E: [email protected]

W: https://kuleuvencongres.be/htc16

Please send any upcoming event

information to Lewis Botcherby at

[email protected]

SWEMSA 2019—Non-Target Screening Embedded in (Open

Access) Platforms and Multi-Disciplinary Applications

The international, interdisciplinary workshop

Solutions and Workflows in (Environmental)

Molecular Screening and Analysis

(SWEMSA 2019) will be held 21–23 October

2019 in the City Hall in Erding, Germany. This

is the second time that this workshop will

be organized close to Munich, which has

one of the largest international airports in Germany. The symposium intends to

continue the exciting international dialogue that started in 2016 at the Non-Target

Conference 2016 in Ascona, Switzerland, and SWEMSA 16 in Garching, Germany,

and has been ongoing in many meetings, workshops, seminars, and conferences.

This workshop will extend the discussion on non-target screening (NTS) with the

following topics:

• Computational mass spectrometry

• NTS in forensics

• NTS in food(omics)

• NTS in metabolomics

• NTS in commercial solutions

• NTS (guideline) in water analysis

• NTS in environmental analysis.

This workshop will bring together leading international scientists from various

consortia. It is the ideal location for industrial and academic researchers

to exchange information with other colleagues from all over the world.

SWEMSA intends to inform, combine, and harmonize the NTS strategies and

workflows from each single discipline to extend the NTS horizon and to offer

the opportunity to “look over the edge”. Participants of various disciplines,

such as chemistry, environment, food, forensic, informatics, metabolomics,

water, and instrumental analysis will discuss the latest developments. The

programme will feature a solution-focused discussion strategy, including

overview talks and panel discussions in each slot. Each panel discussion—a

SWEMSA speciality—is guided and strongly integrates the participants.

The overall aim of this meeting is to condense and harmonize various

common aspects of NTS, to extend the use and understanding of software and

workflow strategies, and to learn about the potential of NTS applied in various

disciplines. The organizers encourage the active participation of younger

scientists in the workshop, and a great amount of effort has been made to

guarantee low participation costs (with registration until 31 August 2019).

A rich scientific and social programme awaits participants with scientific

presentations and discussions and two evening events, respectively. The evening

events will also bring participants closer to the Bavarian lifestyle and offer exciting

culinary delights. Erding offers a wide range of accommodation for all budgets,

and with its international airport it is easily accessible by plane, or by car or train.

The organizers look forward to welcoming delegates in Erding in October.

E: [email protected] W: www.swemsa.eu

Image c

redit:

pure

-life

-pic

ture

s/s

tock

.adobe.c

om

380 LCGC Europe July 2019

EVENTS

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Th

e A

pp

lica

tio

ns B

oo

k

July 2019 | Volume 32 Number 7

www.chromatographyonline.com

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FOOD AND BEVERAGE

383 Analysis of Active Cannabis Compounds in Edible

Food Products: Gummy Bears and Brownies

Olga Shimelis1, Kathy Stenerson1, and Margaret Wesley2, 1MilliporeSigma, 2Pennsylvania State University

MEDICAL/BIOLOGICAL

384 Analysis of Fentanyl and Its Analogues in Human

Urine by LC–MS/MS

Shun-Hsin Liang and Frances Carroll, Restek Corporation

386 Kinase Fragments Dimerize Without Oligomerization

Domains, Shown by SEC-MALS

Thomas Huber, University of Zürich, Department of

Biochemistry

GENERAL

387 Determination of Psilocin and Psilocybin in Magic

Mushrooms Using iHILIC®-Fusion and MS

Tibor Veress1, Norbert Rácz2, Júlia Nagy1, and Wen Jiang3, 1Department of Drug Investigation, Hungarian Institute for

Forensic Sciences, Budapest, Hungary, 2Department of

Inorganic and Analytical Chemistry, Budapest University of

Technology and Economics, Budapest, Hungary, 3HILICON

AB

July | 2019

Volume 32 Number 7

The Applications Book

Image credits: Kwanchaift/stock.adobe.com

Image credits: kenkistler1/stock.adobe.com

Image credits: Pinhead Studio/stock.adobe.com

Image credits: juliasudnitskaya/stock.adobe.com

Image credits: foxaon/stock.adobe.com

Image credits: volgariver/stock.adobe.com

Image credits: likclick/stock.adobe.com

Image credits: pro500/stock.adobe.com

382 LCGC Europe July 2019

CONTENTS

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THE APPLICATIONS BOOK – JULY 2019 383

FOOD AND BEVERAGE

Potency testing in marijuana-infused edibles is a problematic task due

to the complexity of the matrices. The concentration of active ingredients

in edibles can range from a few ppm to 3.5% (1). In this application,

active cannabinoid compounds were extracted from gummy bears (and

also brownies, results not shown), followed by HPLC analysis.

Experimental

Cannabinoid standards (Cerilliant®) used: cannabidivarinic acid

(CBDVA), cannabidivarin (CBDV), cannabigerolic acid (CBGA),

cannabigerol (CBG), cannabidiolic acid (CBDA), cannabidiol

(CBD), tetrahydrocannabivarin (THCV), cannabinol (CBN),

(-)-Δ9-Tetrahydrocannabinol (Δ9-THC), (-)-Δ8-Tetrahydrocannabinol

(Δ8-THC), and (-)-Δ9-Tetrahydrocannabinolic acid A (THCAA). Even

though acidic cannabinoids are not commonly found in edibles, these

were included to demonstrate the ability of the HPLC method to resolve

them from neutral forms, and the method’s potential for testing cannabis

fl owers (which contain acidic cannabinoids).

An Ascentis® Express Biphenyl (2.7 μm particles) HPLC column was

used for separation of all 11 compounds in under 13 min on a standard

pressure HPLC system.

Analysis of Active Cannabis Compounds in Edible Food Products: Gummy Bears and BrowniesOlga Shimelis1, Kathy Stenerson1, and Margaret Wesley2, 1MilliporeSigma, 2Pennsylvania State University

Figure 1: HPLC of orange gummy bear extract at (a) 220 nm and

(b) 280 nm. Peak IDs in Table 1.

Table 1: Recoveries from

spiked gummy bears

Peak

No.Compound

Average

(RSD)

1 CBDVA 91% (2%)

2 CBDV 98% (3%)

3 THCV 90% (3%)

4 CBDA 94% (3%)

5 CBGA 91% (4%)

6 CBD 97% (3%)

7 CBG 96% (4%)

8 CBN 95% (6%)

9 Delta-9-THC 97% (3%)

10 Delta-8-THC 95% (3%)

11 THCA-A 92% (7%)

MerckFrankfurter Strasse 250

Darmstadt, 64293, Germany

Website: www.sigmaaldrich.com

The life science business of Merck

KGaA, Darmstadt, Germany, operates as

MilliporeSigma in the U.S. and Canada

Sample Preparation

Four different bear colours were

tested—orange, yellow, red, and

green. One gummy bear, nonspiked,

(2.3 g) was dissolved in 20 mL of

warm water. This solution was

spiked with cannabinoid (45 ppm

each), and then transferred to a

50-mL QuEChERS extraction tube.

Acetonitrile (10 mL) was added,

followed by 1-min shaking. Supel™

QuE nonbuffered salts (55295-U)

were added, and the samples were

shaken for 5 min followed by 5 min

centrifugation (5000 rpm). The

supernatant was then injected into

the HPLC system (Figure 1).

Results

For all bears, detection was at 220 nm, except for CBDVA due to an

interference from the orange bear; detection was at 280 nm for that

orange bear sample. Excellent recovery values of above 90% were

achieved with good accuracies (Table 1).

Column: Ascentis Express Biphenyl, 10 cm × 2.1 mm i.d., 2.7 μm

Mobile phase: (A) 0.1% TFA in water; (B) 0.1% TFA in acetonitrile

Gradient: 47% B, to 50% B in 13 min, to 100% B in 0.1 min,

100% B for 3 min, to 47% B in 0.1 min, at 47% B

for 2.5 min

Flow rate: 0.70 mL/min

Temp.: 35 °C

Detector: UV, 220 nm & 280 nm (280 nm)

Injection: 5 μL

Pressure: 340 bar

Instrument: Agilent® 1200, with UV detector

Conclusion

The developed HPLC method showed good resolution and can also

be used for analysis of commodities containing acidic cannabinoids;

specifi cally, cannabis fl ower.

Reference

(1) http://analytical360.com/m/archived/216628 (accessed July 2016).

Read the full article at SigmaAldrich.com/ar (Issue 4)

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384 THE APPLICATIONS BOOK – JULY 2019

MEDICAL/BIOLOGICAL

Analysis of Fentanyl and Its Analogues in Human Urine

by LC–MS/MS

Shun-Hsin Liang and Frances Carroll, Restek Corporation

Abuse of synthetic opioid prescription painkillers

such as fentanyl, along with a rapidly growing list of

illicit analogues, is a signifi cant public health problem.

In this study, we developed a simple dilute-and-shoot

method that provides a fast 3.5-min analysis of

fentanyl and related compounds (norfentanyl, acetyl

fentanyl, alfentanil, butyryl fentanyl, carfentanil,

remifentanil, and sufentanil) in human urine by

LC–MS/MS using a Raptor Biphenyl column.

In recent years, the illicit use of synthetic opioids has skyrocketed,

and communities worldwide are now dealing with an ongoing

epidemic. Of the thousands of synthetic opioid overdose deaths

per year, most are related to fentanyl and its analogues. With

their very high analgesic properties, synthetic opioid drugs such

as fentanyl, alfentanil, remifentanil, and sufentanil are potent

painkillers that have valid medical applications; however, they are

also extremely addictive and are targets for abuse. In addition

to abuse of these prescription drugs, the current opioid crisis

is fueled by a growing number of illicit analogues, such as

acetyl fentanyl and butyryl fentanyl, which have been designed

specifically to evade prosecution by drug enforcement agencies.

As the number of opioid drugs and deaths increases, so does

the need for a fast, accurate method for the simultaneous analysis

of fentanyl and its analogues. Therefore, we developed this

LC–MS/MS method for measuring fentanyl, six analogues, and one

metabolite (norfentanyl) in human urine. A simple dilute-and-shoot

sample preparation procedure was coupled with a fast (3.5 min)

chromatographic analysis using a Raptor Biphenyl column. This

method provides accurate, precise identifi cation and quantitation of

fentanyl and related compounds, making it suitable for a variety of

testing applications, including clinical toxicology, forensic analysis,

workplace drug testing, and pharmaceutical research.

Experimental Conditions

Sample Preparation: The analytes were fortifi ed into pooled human

urine. An 80 μL urine aliquot was mixed with 320 μL of 70:30

water–methanol solution (fi vefold dilution) and 10 μL of internal

0.00 0.20 0.40 0.60 0.80 1.00 1.20 1.40 1.60 1.80 2.00 2.20 2.40 2.60 2.80 3.00

Time (min)

Figure 1: The Raptor Biphenyl column effectively separated all target

compounds in urine with no observed matrix interferences. Peak elution

order: norfentanyl-D5, norfentanyl, remifentanil, acetyl fentanyl-13C

6,

acetyl fentanyl, alfentanil, fentanyl-D5, fentanyl, carfentanil-D

5,

carfentanil, butyryl fentanyl, sufentanil-D5, sufentanil.

Table 1: Analyte transitions

Analyte Precursor Ion Product Ion Quantifi er Product Ion Qualifi er Internal Standard

Norfentanyl 233.27 84.15 56.06 Norfentanyl-D5

Acetyl fentanyl 323.37 188.25 105.15 Acetyl fentanyl-13C6

Fentanyl 337.37 188.26 105.08 Fentanyl-D5

Butyryl fentanyl 351.43 188.20 105.15 Carfentanil-D5

Remifentanil 377.37 113.15 317.30 Norfentanyl-D5

Sufentanil 387.40 238.19 111.06 Sufentanil-D5

Carfentanil 395.40 113.14 335.35 Carfentanil-D5

Alfentanil 417.47 268.31 197.23 Acetyl fentanyl-13C6

Norfentanyl-D5

238.30 84.15 — —

Acetyl fentanyl-13C6

329.37 188.25 — —

Fentanyl-D5

342.47 188.27 — —

Sufentanil-D5

392.40 238.25 — —

Carfentanil-D5

400.40 340.41 — —

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THE APPLICATIONS BOOK – JULY 2019 385

MEDICAL/BIOLOGICAL

standard (40 ng/mL in methanol) in a Thomson SINGLE StEP fi lter

vial (Restek cat. #25895). After fi ltering through the 0.2 μm PVDF

membrane, 5 μL was injected into the LC–MS/MS.

Calibration Standards and Quality Control Samples: The calibration

standards were prepared in pooled human urine at 0.05, 0.10,

0.25, 0.50, 1.00, 2.50, 5.00, 10.0, 25.0, and 50.0 ng/mL. Three

levels of QC samples (0.75, 4.0, and 20 ng/mL) were prepared in

urine for testing accuracy and precision with established calibration

standard curves. Recovery analyses were performed on three

different days. All standards and QC samples were subjected to the

sample preparation procedure described.

LC–MS/MS analysis of fentanyl and its analogues was performed

on an ACQUITY UPLC instrument coupled with a Waters Xevo TQ-S

mass spectrometer. Instrument conditions were as follows, and

analyte transitions are provided in Table 1.

Analytical column: Raptor Biphenyl (5 μm,

50 mm × 2.1 mm; cat. #9309552)

Guard column: Raptor Biphenyl EXP guard column

cartridge, (5 μm, 5 mm × 2.1 mm;

cat. #930950252)

Mobile phase A: 0.1% Formic acid in water

Mobile phase B: 0.1% Formic acid in methanol

Gradient Time (min) %B

0.00 30

2.50 70

2.51 30

3.50 30

Flow rate: 0.4 mL/min

Injection

volume: 5 μL

Column temp.: 40 °C

Ion mode: Positive ESI

Results

Chromatographic Performance: All eight analytes were well

separated within a 2.5-min gradient elution (3.5-min total analysis

time) on a Raptor Biphenyl column (Figure 1). No signifi cant matrix

interference was observed to negatively affect quantifi cation of the

fi vefold diluted urine samples. The 5-μm particle Raptor Biphenyl

column used here is a superfi cially porous particle (SPP) column.

It was selected for this method in part because it provides similar

performance to a smaller particle size fully porous particle (FPP)

column, but it generates less system back pressure.

Linearity: Linear responses were obtained for all compounds and

the calibration ranges encompassed typical concentration levels

monitored for both research and abuse. Using 1/x weighted linear

regression (1/x2 for butyryl fentanyl), calibration linearity ranged

from 0.05 to 50 ng/mL for fentanyl, alfentanil, acetyl fentanyl, butyryl

fentanyl, and sufentanil; from 0.10 to 50 ng/mL for remifentanil; and

from 0.25 to 50 ng/mL for norfentanyl and carfentanil. All analytes

showed acceptable linearity with r2 values of 0.996 or greater and

deviations of <12% (<20% for the lowest concentrated standard).

Accuracy and Precision: Based on three independent experiments

conducted on multiple days, method accuracy for the analysis of

fentanyl and its analogues was demonstrated by the %recovery

values, which were within 10% of the nominal concentration for

all compounds at all QC levels. The %RSD range was 0.5–8.3%

and 3.4–8.4% for intraday and interday comparisons, respectively,

indicating acceptable method precision (Table 2).

Conclusions

A simple dilute-and-shoot method was developed for the quantitative

analysis of fentanyl and its analogues in human urine. The analytical

method was demonstrated to be fast, rugged, and sensitive with

acceptable accuracy and precision for urine sample analysis. The

Raptor Biphenyl column is well suited for the analysis of these

synthetic opioid compounds and this method can be applied to

clinical toxicology, forensic analysis, workplace drug testing, and

pharmaceutical research.

Restek Corporation110 Benner Circle, Bellefonte, Pennsylvania 16823, USA

Tel. 1 (814) 353 1300

Website: www.restek.com

Table 2: Accuracy and precision results for fentanyl and related compounds in urine QC samples

Analyte

QC Level 1 (0.750 ng/mL) QC Level 2 (4.00 ng/mL) QC Level 3 (20.0 ng/mL)

Average Conc.

(ng/mL)

Average %

Accuracy %RSD

Average Conc.

(ng/mL)

Average %

Accuracy %RSD

Average Conc.

(ng/mL)

Average %

Accuracy %RSD

Acetyl fentanyl 0.761 102 1.54 3.99 99.7 2.08 19.9 99.3 0.856

Alfentanil 0.733 97.6 3.34 3.96 98.9 8.38 20.9 104 6.73

Butyryl fentanyl 0.741 98.9 6.29 3.77 94.3 6.01 20.8 104 4.95

Carfentanil 0.757 101 7.34 3.76 94.0 4.64 20.6 103 4.24

Fentanyl 0.761 102 1.98 3.96 99.1 2.31 19.9 99.6 1.04

Norfentanyl 0.768 103 6.50 4.04 101 1.84 20.1 101 2.55

Remifentanil 0.765 102 3.42 3.97 99.2 3.68 20.8 104 4.14

Sufentanil 0.752 100 1.67 3.93 98.3 1.28 20.1 100 0.943

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386 THE APPLICATIONS BOOK – JULY 2019

MEDICAL/BIOLOGICAL

Kinase Fragments Dimerize Without Oligomerization Domains, Shown by SEC-MALSThomas Huber, University of Zürich,

Department of Biochemistry

Determination of oligomeric states is an important issue in protein

chemistry. For example, self-assembly via oligomerization domains

is crucial for the regulation of several protein kinases. Determination

of the oligomeric state of fragments of these kinases is a means of

verifying the involvement of each domain in self-assembly.

Analytical size-exclusion chromatography (SEC) is widely used for

determining molar mass and oligomeric state of proteins in solution,

but it exhibits some important limitations. For example, interactions

of proteins with column material can lead to delayed elution and

hence erroneous results when relying on column calibration. Since

even ideal elution occurs according to hydrodynamic size rather

than true molecular weight, there are no appropriate molar mass gel

fi ltration standards for analysis of proteins, fragments, or complexes

of non-globular structure that present a different size or molecular

weight dependence than globular proteins.

The use of size-exclusion chromatography in combination with

multi-angle light scattering (SEC-MALS) determines molecular weights

independently of elution time and conformation, overcoming the need

for standards and the errors inherent in analytical SEC. In SEC-MALS,

chromatography is used solely to separate the individual species so they

can be characterized by light scattering for biophysical properties such

as molar mass, size, conformation, and degree of conjugation.

This note describes the analysis of a kinase fragment lacking its

association domain in order to determine its oligomeric state in solution.

SEC-MALS revealed that the kinase moiety clearly remains dimeric in

solution, even in the absence of its purported oligomerization domain.

Experimental Conditions

An HP-SEC column was calibrated using bovine serum albumin (BSA)

monomer and dimer. The kinase fragment and alcohol dehydrogenase

(ADH, 38 kDa monomer and 150 kDa tetramer) were each run on the

column, and the elution times compared to those of BSA monomer

(66.4 kDa) and dimer (133 kDa). Absolute molar mass (MW) of the

proteins at each elution volume were determined by analysis of signals

from the multi-angle light scattering and refractive index detectors

(DAWN and Optilab, respectively) in ASTRA software. Chromatograms

were overlaid with molecular weight values calculated for each elution

time along the peaks, as seen in Figure 1.

Results and Discussion

The monomeric kinase fragment has a sequence molar mass of

53.5 kDa. The fragment (red trace) eluted at nearly the same volume

as the BSA dimer (blue trace), suggesting that its molar mass is

approximately 140 kDa, or trimeric. However, MALS determines an

absolute molar mass in solution of 108 kDa, revealing that the protein

Wyatt Technology Corp.6330 Hollister Ave, Santa Barbara, California 93110, USA

Tel.: 1 (805) 681 9009

Website: www.wyatt.com

Figure 1: Molar mass, as determined by multi-angle light scattering,

vs. elution volume of kinase fragment (red), bovine serum albumin

(BSA, blue), and alcohol dehydrogenase (ADH, green). Molar masses

deduced from the elution volumes of kinase fragment and ADH are

shown to be misleading when compared with absolute molar masses

from SEC-MALS.

is actually a dimer. The molecular weight is absolutely uniform across

the peak, indicating a high degree of homogeneity. Such early elution is

indicative of a non-globular conformation.

ADH tetramer (green trace, 150 kDa) eluted between the monomer

and dimer of BSA, possibly because of ADH-column interactions that

caused it to elute late relative to its size. Comparison of the fragment’s

elution volume to ADH monomer and tetramer would mislead the

investigator to assume a tetrameric state, even further removed from

the truth than comparison to BSA.

Conclusions

SEC-MALS provides true solution molecular weight for proteins,

overcoming the inherent errors produced by reliance on column

calibration. Here we have shown by SEC-MALS that kinase

fragments are dimeric, even without the purported oligomerization

domain; but they are not trimeric or tetrameric as might have

been deduced via column calibration. The addition of a DAWN

MALS detector to standard SEC reveals the essential biophysical

properties of proteins, fragments, and complexes.

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THE APPLICATIONS BOOK – JULY 2019 387

GENERAL

Determination of Psilocin and Psilocybin in Magic Mushrooms Using iHILIC®-Fusion and MSTibor Veress1, Norbert Rácz2, Júlia Nagy1, and Wen Jiang3, 1Department of Drug Investigation,

Hungarian Institute for Forensic Sciences, Budapest, Hungary, 2Department of Inorganic and Analytical

Chemistry, Budapest University of Technology and Economics, Budapest, Hungary, 3HILICON AB

Hallucinogenic mushrooms, known as magic mushrooms, contain

psychoactive compounds such as psilocin and psilocybin (Figure 1).

This hallucinogenic effect means they are constantly offered on

the black market. Therefore, the reliable quantifi cation of these

compounds is a particularly important task for forensic analysis

because their results have a signifi cant impact on the judgement

passed by the courts.

Although there are many analysis methods available in forensic

laboratories and in the scientific literature, the majority of them are

based on reversed-phase liquid chromatography (LC) separation

(1–6). Due to the highly hydrophilic nature of psilocybin and psilocin,

reversed-phase LC is not able to provide sufficient retention for them.

Moreover, it is crucial to develop new methods and techniques that

can improve the analysis detectability, selectivity, and productivity.

To fulfill these goals, the application of hydrophilic interaction liquid

chromatography (HILIC) and mass spectrometry (MS) is investigated.

In this study, we aimed to use a charge modulated iHILIC®-Fusion

HILIC column for the analysis of extracts from hallucinogenic

mushrooms and evaluate its potential for forensic application.

Experimental

LC–MS System: Agilent 1100 LC system and Bruker Esquire 6000

ion trap mass spectrometer, operated in positive ionization mode

(ESI+). Chromatographic data were acquired and evaluated with

ChemStation Rev. A. 10.02.

Column: 150 × 4.6 mm, 3.5-μm 100 Å iHILIC®-Fusion (P/N

110.154.0310, HILICON AB, Sweden)

Mobile Phase: 80:20 (v/v) acetonitrile–ammonium format (10 mM,

pH 3.5)

Flow Rate: 0.5 mL/min

Column Temperature: 12 °C

Sample Preparation: Quasi-counter current extraction with methanol

at 60 °C in a Shimadzu 10/A HPLC system. A 50-mg measure of

air-dried and homogenized hallucinogenic mushroom was fi lled in

the extractor chamber (an empty 250 × 4.6 mm HPLC column).

The standard solutions were 5 μg/mL and 500 μg/mL for psilocin

and psilocybin, respectively. Methanol was used as the solvent.

Injection Volume: 1 μL

Results and Discussion

In our previous study (2), the methanolic mushroom extract was

fi rst separated under the conditions within a designed experimental

space with a total of 18 model establishment points and two

approval points, considering the mobile phase composition, pH, and

temperature. The factors that affect the separation selectivity and

resolution on three iHILIC® columns were studied using DryLab®

and STATISTICA®. It was found that iHILIC®-Fusion provides

best separation regarding separation selectivity and effi ciency.

Figure 2 illustrates the separation of mushroom extract and also

HN

(a) (b)

HN

NN

OH

OHHO

OO

P

Figure 1: Chemical structures of (a) psilocin and (b) psilocybin.

1.1E+6

1.0E+6

9.0E+5

8.0E+5

7.0E+5

6.0E+5

5.0E+5

4.0E+5

3.0E+5

2.0E+5

1.0E+5

0.0E+0

0 1 2 3 4 5 6 7 8 9 10

Time (min)

11 12 13 14 15

0 1 2 3 4 5 6 7 8 9 10

Time (min)

11 12 13 14 15

0 1 2 3 4 5 6 7 8 9 10

Time (min)

11 12 13 14 15

TIC (Mushroom extract)

m/z 205 (Psilocin)

m/z 285 (Psilocybin)

Inte

nsi

ty

9.0E+5

8.0E+5

7.0E+5

6.0E+5

5.0E+5

4.0E+5

3.0E+5

2.0E+5

1.0E+5

0.0E+0

Inte

nsi

ty

9.0E+5

8.0E+5

7.0E+5

6.0E+5

5.0E+5

4.0E+5

3.0E+5

2.0E+5

1.0E+5

0.0E+0

Inte

nsi

ty

Figure 2: Total ion chromatogram (m/z 40–400) of the methanolic

mushroom extract and extracted ion chromatograms of m/z 205

(psilocin) and m/z 285 (psilocybin).

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388 THE APPLICATIONS BOOK – JULY 2019

GENERAL

the extract ion chromatograms at m/z 205 (psilocin) and m/z 285

(psilocybin), respectively. It is clear that iHILIC®-Fusion was able to

separate psilocin and psilocybin from each other and also from the

major matrix compounds within 15 min. An unique feature is that

psilocybin elutes with a retention factor two times greater than that

of psilocin. In addition, the sample preparation consists of few steps

to minimize error sources and assure reliable results.

In the second step of this work, we separated the methanolic

solution of psilocin and psilocybin standards to confirm the detection

of these two alkaloids in the mushroom extract. As shown in Figure 3,

both psilocin and psilocybin have identical retention times to the

standards compared to those peaks from the mushroom extracts.

Therefore, the developed method is selective for the two target

compounds and can be used for the quantification as described in

our early work (1).

Conclusion

This work illustrates how to use an iHILIC®-Fusion column and

MS detection to separate and identify psilocin and psilocybin in

hallucinogenic mushrooms or ”magic mushroom” extracts. This

developed HILIC–MS method can be utilized in forensic and clinical

applications.

References

(1) J. Nagy and T. Veress, J. Forensic Res. 7, 356 (2016), DOI: 10.4172/2157-

7145.1000356.

(2) N. Rácz, J. Nagy, W. Jiang, and T. Veress, J. Chromatogr. Sci. 57, 230–237

(2019).

(3) M.W. Beug and J. Bigwood, Journal of Chromatography 207, 379–385

(1981).

(4) N. Anastos, S.W. Lewis, N.W. Barnett, and D.N. Sims, J. Forensic Sci. 51,

45–51 (2006).

(5) R. Kysilka and M. Wurst, Planta Med. 56, 327–328 (1990).

(6) V. Gambaro, G. Roda, G.L. Visconti, S. Arnoldi, and E. Casagni, J. Anal.

Bioanal. Tech. 6, 277 (2015).

HILICON ABTvistevägen 48, SE-90736, Umeå, Sweden

Tel.: +46 (90) 193469

E-mail: [email protected]

Website: www.hilicon.com

3.5E+6

2.8E+6

2.1E+6

1.4E+6

7.0E+5

0.0E+0

0 1 2 3 4 5 6 7 8 9 10

Time (min)

11 12 13 14 15

0 1 2 3 4 5 6 7 8 9 10

Time (min)

11 12 13 14 15

0 1 2 3 4 5 6 7 8 9 10

Time (min)

11 12 13 14 15

0 1 2 3 4 5 6 7 8 9 10

Time (min)

11 12 13 14 15

TIC (Psilocin)

TIC (Psilocybin)

Inte

nsi

ty

3.5E+6

2.8E+6

2.1E+6

1.4E+6

7.0E+5

0.0E+0

Inte

nsi

ty

4.0E+6

3.0E+6

2.0E+6

1.0E+6

0.0E+0

Inte

nsi

ty

4.0E+5

3.5E+5

3.0E+5

2.5E+5

2.0E+5

1.5E+5

1.0E+5

5.0E+4

0.0E+0

Inte

nsi

ty

m/z 205 (Psilocin)

m/z 285 (Psilocybin)

Figure 3: Total ion chromatogram (m/z 40–400) of psilocin and

psilocybin standards and extracted ion chromatograms of m/z 205

(psilocin) and m/z 285 (psilocybin).

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PRESS PARTNERS

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