gohsenoltm eg series - pharmtech-expo.ru · pdf fileexcipient binder pressure, tableting ......

The Nippon Synthetic Chemical Industry Co.,Ltd Basic Products Segment Acetyl and Fine Chemicals Dept.

http://www.gohsenol.com

GOHSENOLTM EG series

Highly Purified Polyvinyl Alcohol

for Pharmaceutical Excipients



CONTENTS

Overview of GOHSENOLTM EG 4

Product List

List (1) Granule Type 5

List (2) Powder Type 6

Dissolution Method 7

Regulatory Information 8

Major Applications

Representative Applications 9-10

Film Properties

Comparison with Other Excipients 11-12

Impurities Information

Metal elements 13

Peroxides 14



Application Examples

Binder (Tablet) 16-18

Film Coating Agent (Tablet) 19-20

Gel Patch 21

Thickener （Ophthalmic / Nasal Solution） 22

Other Application 23

For Inquiries / Sample Request 24

CONTENTS



What is GOHSENOLTM EG ？

“GOHSENOLTM EG” is a highly purified polyvinyl alcohol

(PVA) . All grades comply with major pharmacopoeias.

Chemical Structure

Pharmacopoeia conformable to United States Pharmacopoeia (USP)

European Pharmacopoeia (EP)

Japanese Pharmaceutical Excipients (JPE)

CH2-CH CH2-CH

OH OCOCH3 m n m+n=100

Overview



GOHSENOLTM EG

Granule Type

Products

Degree of

Hydrolysis

[mol%]

Viscosity *1, *2

(Center value)

[mPa・s]

Main applications

EG-03P

86.5-89.0

3.0-3.8 (3.4) Emulsifier, Granulating Agent

EG-05P 4.8-5.8 (5.3) Binder, Granulating Agent, Base of OD Film

EG-18P 16.0-20.0 (18.0) Binder

EG-22P 20.0-24.5 (22.3) Binder

EG-30P 27.0-33.0 (30.0) Gel Patch

EG-40P 40.0-46.0 (43.0) Ophthalmic Solution, Emulsifier

EG-48P 45.0-52.0 (48.5) Ophthalmic Solution

*1. 4% aqueous solution at 20 ℃

*2. indicated as general values. We have viscosity standards fulfilling

requirements of USP, EP and JPE.

Product List (1)



GOHSENOLTM EG

Powder Type

Products

Degree of

Hydrolysis

[mol%]

Viscosity *1, *2

(Center value)

[mPa・s]

Main application

EG-05PW

86.5-89.0

4.8-5.8 (5.3) Binder, Film Coating Agent

EG-30PW 27.0-33.0 (30.0) Gel Patch, Ophthalmic Solution

EG-40PW 40.0-46.0 (43.0) Binder

*1. 4% water solution at 20 ℃

*2. indicated as general values. We have viscosity standards fulfilling

requirements of USP, EP and JPE.

Product List (2)



Dissolution Method

Add GOHSENOLTM EG slowly to water while stirring

continuously. After dispersing evenly,

heat the solution to 80-90 ℃ and keep it for 30-60

minutes until complete dissolution.（※1, ※2）

※1. Avoid rising temperature rapidly, which may cause

foaming.

※2. Adding GOHSENOLTM EG at one time may create the

residue and worsen its solubility.

How to Use



CAS No. 25213-24-5

HS Code. 39053000

JPE*1 Self-Imposed GMP No. GAB 0130001

Drug Master File (Type Ⅳ) No.26119

COS/CEP under registration

The following Certificates / Statements available

Regulatory Information

BSE/TSE Free Radiation Free

OVI Free Melamine Free

Gluten Free Allergens statement

GMO Free Residual Solvent

Endotoxins*2 Microbiological test*2

*1 Japanese Pharmaceutical Excipients

*2 available on request



Target Area

Solid formulation

Binder

Granulation Agent

Film Coating Agent

Base of OD Film

Low viscosity types have better cold water solubility.

EG-05PW type is suitable for binder, granulating agent and film coating agent.

PVA offers taste-masking property and better stability of API’s

Example (Image)

Introduction to Application examples

API

Excipient

Binder

Pressure,

Tableting

Film Coating



Target Area

Non-Solid formulation

Gel Patch

Thickener

Emulsifier

Dispersing Agent

High viscosity types offer better dispersion and adhesive strength.

Therefore, these grades are suitable for tackifier for Gel Patch.

PVA has surfactant ability, it is used for the production of sustained-release

Injection and Ophthalmic medicine and Nasal solution.

Example (Image)

Water Soluble Polymers

Excipient

Preparation

Plaster

Release film

(Liner sheet)

Base

Introduction to Application examples



Physical properties

*1. Polyvinyl Alcohol : GOHSENOLTM EG-05PW

*2. 4% aqueous solution

Properties Unit

Polyvinyl Alcohol

(PVA)*1

Hydroxypropyl

Cellulose

(HPC)

Hydroxypropyl

Methyl Cellulose

(HPMC)

Viscosity*2 mPa･s 4.9 49.0 11.1

Tensile strength MPa 119.4 5.1 46.9

Linear expansion % 188.4 103.4 102.7

Young modulus MPa 672 419 2,251

＜Comparison between excipients (1)＞

Film Properties

GOHSENOLTM EG series excels HPMC and HPC

in adhesion, film strength and elongation.



Gas and water vapor barrier ability

PVA film offers excellent oxygen and water vapor barrier properties.

Properties

Polyvinyl

Alcohol

(PVA)*1

Hydroxypropyl

Cellulose

(HPC)

Hydroxypropyl

Methyl Cellulose

(HPMC)

Transmision rate

of O2 gas*2

(cc/m2･day・atm)

25℃ 60%RH 0.7 128 152

40℃ 75%RH 18 > 200 > 200

Transmission rate

of water vapor*3

(g/m2･day・atm)

25℃ 60%RH 3 95 186

40℃ 75%RH 85 470 740

＊１ Grades ： GOHSENOLTM EG-05PW

Film thickness ： 100μm (made by method of Pool cast）

＊２ Measuring machine of transmission of the O2 gas ： OXTRAN2/20

＊３ The method of transmission of water vapor ： Comply with JIS Z 0208

＜ Comparison between excipients (2)＞

Film Properties



Metal impurities

We have analyzed for 14 metals based on the EMA

guideline.

PVA is far below the detection limit. (N.D.)

Method of Analysis ：Inductively-Coupled Plasma Mass Spectrometer 〔ICP-MS〕

Grades ： GOHSENOLＴＭ EG-05P, EG-48P

Classification (Metal element）

Result EMA Guidelines

Oral Parenteral

Conc.

(ppm)

PDE

[μg/day]

Conc.

(ppm)

PDE

[μg/day]

Conc.

(ppm)

Class 1A (Pt, Pd) < 0.2 100 10 10 1

Class 1B （Ir, Rh, Ru, Os) < 0.2 100 10 10 1

Class 1C (Mo, Ni, Cr, V) < 0.5 250 25 25 2.5

Class 2 (Cu, Mn) < 5 2,500 250 250 25

Class 3 (Fe, Zn) <26 13,000 1,300 1,300 130

Impurities information



Grade Result of analysis

EG-05PW <0.1meq *1

expressed as H2O2 NMT 3.4ppm

*1 Method of Analysis : AOCS (American Oil Chemists’ Society) Cd 8-53

Detection limit : 0.1meq/kg

Impurities information

Peroxides

Peroxides are contained in the other pharmaceutical

additives, but not in PVA.

PVP

（Polyvinyl

pyrrolidone）

NMT 400 ppm

expressed as H2O2

Reference ( The specification of residual peroxide of PVP in USP 37 ）



Application Information



Formulation Classification F1 F2 F3

Metformin hydrochloride API 77

Microcrystalline Cellulose Excipient 15

PVA (EG-05PW)

Binder

5 - -

PVP (K-30) - 5 -

PVP (K-90) - - 5

Croscarmellose Sodium Disintegrant 2

Magnesium Stearate Lubricant 1

Total 100 [wt%]

Binder (Tablet)

Formulation table

3-5% of PVA are generally formulated.



Physical properties F1 F2 F3

Binder PVA

(EG-05PW)

PVP

(K-30)

PVP

(K-90)

Angle degree of repose 25.7 29.8 29.6

Bulk density [g/ml] 0.420 0.416 0.376

Tap density [g/ml] 0.53 0.56 0.48

Carr’s Index 20.9 25.3 21.4

Hausner Ratio 1.27 1.34 1.27

Moisture content [%] 3.7 3.2 2.5

Physical properties

Granules show suitable physical properties for binders.

Binder (Tablet)



Physical properties

EG-05PW dissolves in water as fast as K-30 does.

Physical properties F1 F2 F3

Binder PVA

(EG-05PW)

PVP

(K-30)

PVP

(K-90)

Weight [mg] 649.5±3.8 651.4±3.3 652.0±3.7

Thickness [mm] 4.61±0.024 4.63±0.01 4.70±0.012

Hardness [kg/cm2] 6.16±0.408 5.91±0.580 5.58±0.370

Friability [%] 0.36 0.32 0.31

Disintegration time [min] 1.71±0.30 2.26±0.12 12.96±0.40

Drug Content (%) 102.2±5.7 103.0±1.7 101.5±0.64

Binder (Tablet)



PVA normally comprises 15-20% of a film coating agent.

Because PVA has high tacking property compared to HPMC, it is recommended

to add anti-tacking agents such as talc.

Formulation EG-05PW HPMC

Viscosity of 4% water solution (mPa・s) 4.9 11.1

Coating agent EG-05PW 10 -

HPMC - 10

Plasticizer PEG 1500 1 ←

Anti-tacking agent Talc 0.2 ←

Opacifier Titanium Dioxide 0.2 ←

Solvent Water q.s. ←

Film Coating Agent (Tablet)

Formulation table



Film Coating Agent (Tablet)

コーティング量は、３～５％が好適です。

バリヤ性を付与する場合のコーティング量は、多めに設定してください。

Physical properties Uncoated

Tablet EG-05PW HPMC

Cast film

Thickness [mm] - 0.11±0.01 0.18±0.01

Diametral crushing

Strength [kg/cm2] 5.4 - -

Friability [%] 0.26 - -

Disintegration

time [sec] 43 58 171

Weight

Gain [%] - 4.4 7.1

Physical properties



Content Quantity [%]

HPC-M 2

API 2

Gelatin 22

PVA 5

Glycerin 30

Kaolin clay 17

Polyacrylic sodium 1

Polybutene 3

Water 18

Total 100

Gel Patch

• GOHSENOLＴＭ EG has

adhesion to the release

film, excellent solubility

and dispersibility of API.

• Various grades of

GOHSENOLＴＭ EG are

used for Gel Patches.

＜Example＞

Formulation table



Thickener （Ophthalmic / Nasal）

A formulation example as a Thickener

GOHSENOLTM EG is used for eyedrops and nasal

drops as thickeners or dispersants.

PVA content is normally between 0.1 to 1.4%.

＜Example of the formulated APIs with PVA＞



Other Applications

Other Applications

• Sustained-release Injection :

PVA is used in producing microspheres as

a dispersion stabilizer.

• Orally Disintegrating Film :

PVA is used as a thin-film for oral drugs.

PVA is used for various uses such as

powder medicines (granules), external

preparations (ointments) and culture media.



Thank you for your attention.

The Nippon Synthetic Chemical Industry Co., Ltd.

Acetyl and Fine Chemicals Dept.

Basic Products Segment

Shibaura Renasite Tower,

9-1, Shibaura 3-chome, Minato-ku, Tokyo,

108-0023, Japan

TEL : +81-3-6436-2813

FAX : +81-3-6436-2820

Sample bottle

Content : 500g

gohsenoltm eg series - pharmtech-expo.ru · pdf fileexcipient binder pressure, tableting ......

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