1 Technical Information SYLOID ® XDP Silica Pharmaceutical Excipients Solutions for Liquisolid and Lipid-based Formulations SYLOID ® XDP silicas are meso-porous, 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). 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. 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. Internal Surface Area Oils are retained in the internal pore structure External Surface Area The Benefits of SYLOID ® XDP Silica SYLOID ® XDP silica can effectively transform liquid formulations into stable solid dosage forms, offering benefits such as: • Serves as a solid carrier for lipid-based drug delivery systems • Transforms liquids to easy-to-handle solids • Improves bioavailability of oily actives • Increases API loading into solid dosage forms • Releases API quickly and completely from solid dosage forms • Creates liquisolid formulations • Is inert and has a minimum of interactions with APIs (meets the test requirements in global monographs) Volumetric Oil Absorption* g oil/ml MCC SYLOID ® XDP Silica PPT Silica Talc Dicalcium Phosphate Micronized SG Fumed Silica 0.0 0.2 0.4 0.6 0.8 *Testing based on over 20 different oils, lipids and co-solvent surfactants. Results are available upon request.
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Technical Information
SYLOID® XDP Silica Pharmaceutical Excipients Solutions for Liquisolid and Lipid-based Formulations
SYLOID® XDP silicas are meso-porous, 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).
Oil Adsorption CapacityThe 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. 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.
Internal Surface Area
Oils are retained in the internal pore structure
External Surface Area
The Benefits of SYLOID® XDP Silica SYLOID® XDP silica can effectively transform liquid formulations into stable solid dosage forms, offering benefits such as:
• Serves as a solid carrier for lipid-based drug delivery systems
• Transforms liquids to easy-to-handle solids
• Improves bioavailability of oily actives
• Increases API loading into solid dosage forms
• Releases API quickly and completely from solid dosage forms
• Creates liquisolid formulations
• Is inert and has a minimum of interactions with APIs (meets the test requirements in global monographs)
Volumetric Oil Absorption*
g oil/ml
MCC
SYLOID® XDP Silica
PPT Silica
Talc
Dicalcium Phosphate
Micronized SG
Fumed Silica
0.0 0.2 0.4 0.6 0.8
*Testing based on over 20 different oils, lipids and co-solvent surfactants. Results are available upon request.
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ProcedureMost 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
No Solvent Required
No Drying Needed
Dissolution Profile for solid SEDDSLiquid 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.
Liquid SEDDS SYLOID® XDP Silica API
00 20 40 60 80 100 120
20
40
60
80
100
120
Time (m)
Dis
solu
tion
%Comparison of Loadability in a Zero Size CapsuleSYLOID® XDP silica allows the highest loading and maximum filling amount in a standard capsule.
SYLOID® XDPSilica
GranulatedFumed Silica
MagnesiumAluminum Silicate
SYLOID® FPSlica
0
50
100
150
200
250
300
350
400
450
500 Max. Filling Amount (mg of 1.5:1 load)
Max
Fill
Am
ou
nt i
n m
g
Release of Loaded Oils ComparisonSYLOID® XDP silica provides the most complete release of loaded oils.
SYLOID® XDPSilica
GranulatedFumed Silica
MagnesiumAluminum Silicate
0
10
20
30
40
50
60
70
80
90
100 Sesame Oil
Miglyol 812
Tocopherol*
% O
il R
elea
se
*In vitro dissolution by USPII apparatus & analyzed by HPLC:
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.
