syloid xdp silica...oil-based formulations is converting oily solutions and liquid formulations into...
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Optimized for Liquisolid and Lipid-based FormulationsSyloid® XDP silicas are mesoporous, amorphous, silica gel excipients with a unique morphology that create an excellent solid porous carrier for pharmaceutical formulations. The combined adsorption capacity, porosity, particle size, and density provides a tool to create formulations which can expedite manufacturing and improve efficacy of the final dosage form.
Lipids are increasingly being used in formulations today as drug solubilizers, adsorption enhancers and vehicles for lipid based drug delivery, in order to increase the oral bioavailability of poorly soluble drugs. While oily actives continue to be discovered, the main challenge in oil-based formulations is converting oily solutions and liquid formulations into compressible solid or semi-solid formulations.
Syloid® XDP silicas has been specifically designed for converting lipids, oily drugs, and drugs in oil solutions into free flowing powders. They can be effective as adsorbents in techniques such as solid dispersion, semi-solids and in lipid-based technologies such as self-emulsifying drug delivery systems (SEDDS).
Syloid® XDP Silicas Oil Adsorption Capacity The combined internal and external porosity of Syloid® XDP silicas allow a greater surface area and a higher adsorptive capacity for oils, lipids and liquids that are commonly used for solubilizing and loading APIs.
External Surface Area
Oils are retained in the internal pore structure
Internal Surface Area
Volumetric Adsorption Comparison*
In volume constrained systems such as capsules and tablets, carriers must be able to deliver the largest amount of liquid per volume. With the best balance of absorption capacity and density, SYLOID® XDP silica provides optimum loadability.
SYLOID® XDP SilicaPharmaceutical Excipient
n Increase API loading in solid dosage forms
n Release API quickly and completely from solid dosage forms
n Create liquisolid formulations
n Solid carrier for lipid-based drug delivery systems
n Transform liquids to easy to handle solids
n Improve bioavailability of oily actives
Syloid® XDP silica benefits:
*Testing based on over 20 different oils, lipids and co-solvent surfactants. Results are available upon request.
Syloid® XDP silicas meet the test requirements in global monographs. Because it is silica, it is inert and has a minimum of interactions with the API.
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SYLOID® XDP MCC PPT Silica Talc Dicalcium Phosphate
Micronized SG Fumed Silica
g oil /ml
Syloid® XDP Silica
MCC PPT Silica Talc Dicalcium Phosphate
Micronized SG
Fumed Silica
g oi
l/ m
l
10/13 M458
No Drying Needed
No Solvent Required
Syloid® XDP silica can be used as carriers for adsorbing large amounts of oils and other liquids, thus converting oils to powders with optimum density while maintaining good flow properties, maximum loading in capsules and tablets, and maximum release with and without surfactants.
Syloid® XDP Silica allows the highest loading and maximum filling amount in a standard capsule.
Comparison of Loadability in a Zero Size Capsule
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GRACE® and SYLOID® are trademarks, registered in the United States and/or other countries, of W. R. Grace & Co.-Conn. VISIONHT® is a trademark,registered in the United States and/or other countries, of Alltech Associates, Inc. ROCKET™ is a trademark of Alltech Associates, Inc. WATERS® is a trademark of Waters Investment. Ltd. This trademark list has been compiled using available published information as of the publication date of this brochure and may not accurately reflect current trademark ownership or status. Alltech Associates, Inc. is a wholly owned subsidiary of W. R. Grace & Co.-Conn. Grace Discovery Sciences is a product group of W. R. Grace & Co.-Conn. Grace Materials Technologies is a business segment of W. R. Grace & Co.-Conn. which includes products formerly sold under the Alltech and Grace Davison brand. © Copyright 2013 W. R. Grace & Co.-Conn. All rights reserved.
The information presented herein is derived from our testing and experience. It is offered for your consideration and verification. Since operating conditions vary significantly, and are not under our control, we disclaim all warranties on the results that may be obtained from the use of our products. W. R. Grace & Co.-Conn. and its subsidiaries can not be held responsible for any damage or injury occurring as a result of improper installation or use of its products. Grace reserves the right to change prices and/or specifications without prior notification.
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10/13 M458
Dissolution Profile for solid SEDDS
Most carriers require the use of solvents to load the lipid, followed by drying. The unique morphology of Syloid® XDP silica allows lipid systems to be directly loaded onto the material, eliminating solvent use and drying, simplifying the liquid to solid transformation.
➡Lipid-based formulation
Syloid® XDP Silica ➡
Free-flowing
liquisolid
Procedure for Liquisolids Using Syloid® XDP Silicas without Solvents
Liquid SEDDS can be easily transformed to a solid powder by loading onto Syloid® XDP silica. SEDDS formulation loaded on Syloid® XDP silica, can provide an equivalent API release provide as the liquid formulation.
Contact your local Grace Representative to request a sample of Syloid® XDP Silica, or for more information.
Syloid® XDP silica provides the most complete release of loaded oils.
*In vitro dissolution by USPII apparatus & analyzed by HPLC:
Column: Grace® VisionHT® HL Rocket™ C18 Column, 53x7mm, 3µm System: Waters® UPLC Instrument Wavelength: 294nm Moblie Phase: 85% ACN, 10% MeOH, 5% H20
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Dis
solu
tion
%
Time (m)
Dissolution Profile
Liquid SEDDS
Solid SEDDS (XDP)
API
Liquid SEDDS
Syloid® XDP Silica
API
Dis
solu
tion
%
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S1 Silica GFS MAS Syloid® 244 FP
Max. Filling Amt (mg) in Zero size capsules
Max. Filling Amt (mg of 1.5:1 load)
Max
Fill
Am
ount
in m
g
Syloid® XDP Silica
Syloid® FP Silica
Max
Fill
Am
ount
in m
g
Syloid® XDP Silica
Granulated Fumed Silica
Syloid® FP Silica
Magnesium Aluminum Silicate
Max. Filling Amt (mg of 1.5:1 load)
Release of Loaded Oils Comparison
Syloid® XDP Silica
Granulated Fumed Silica
Magnesium Aluminum Silicate
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SYLOID® XDP Silica
Granulated Fumed Silica
Magnesium Aluminum Slicate
% O
il R
elea
se
Sesame oil
Miglyol 812
Tocopherol
Sesame Oil
Miglyol 812
Tocopherol*%
Oil
Rel
ease