AEROPERL® 300 Pharma

What is AEROPERL® 300 Pharma Mesoporous Silica?

AEROPERL® 300 Pharma is a mesoporous silica obtained by granulating colloidal

silicon dioxide. Mesoporous silicas are of great interest in the pharmaceutical industry
due to their unique properties, such as ordered pore structures, very high internal
surface areas and availability in a variety of shapes and morphologies (spheres, rods
and powders).

Scanning electron micrograph of AEROPERL® 300 Pharma

AEROPERL® 300 Pharma is a granulated high purity colloidal silicon dioxide for use in
pharmaceutical products (tested according to USP/NF and Ph. Eur. Monograph 0434).

Physicochemical Properties AEROPERL® 300 Pharma Mesoporous Silica

Specific surface area (BET) m2/g 260 – 320

pH 3.5 – 5.5
Tapped density (g/l) ≈270
Average particle size (µ) 26 – 60
Pore volume (ml/g) 1.5 – 1.9
Shape Speherical

SCOPE

Applications Pharmaceuticals Carrier for liquid and pasty (active) ingredients

Increases the dissolution of poorly soluble Active Pharmaceutical Ingredients (APIs)
Desiccant for Moisture Activated Dry Granulation (MADG) processes.

Feature

Properties Easy handling, low dust High purity Excellent flow behaviour both loaded
and unloaded
APPLICATION

Direct Compression; Dry Granulation; Wet Granulation; Immediate Release

Tablets; Orally Dissolving Technology; Chewables; Capsules; Power Blends

How is AEROPERL® 300 Pharma Mesoporous Silica used in Formulations?

Improving the Bioavailability of Poorly Water Soluble Drug Molecules

For poorly soluble active pharmaceutical ingredients (BCS II and IV) increasing the
effective surface area in contact with the dissolution medium can enhance the rate of
drug dissolution and improve bioavailability. This can be achieved by loading the
drug substance in the form of small crystallites onto AEROPERL® 300 Pharma
surface. Alternatively, the drug substance can be dissolved into a lipid carrier which is
then adsorbed onto the mesoporous silica surface. Both these approaches result into a
homogeneous and reproducible drug-loading and release.

Conversion of Liquid Lipid Formulations into Powders

Owing to its porous and highly adsorptive properties, AEROPERL® 300 Pharma can
be used to change lipid formulations into powders. It is possible to use the material as
a carrier and load it with up to 150% of its own weight with an oil without
compromising its powder flow properties. This is undertaken via a simple blending
process without the need for specialised equipment.

The high capillary forces draw the liquid into the pores. Moreover, this is a purely
physical phenomenon, meaning that polarity of the lipid does not impact on
adsorption – so provided the oil has reasonable viscosity, it will be adsorbed.

Inorganic Solid Dispersions via Solvent Evaporation Technique

AEROPERL® 300 Pharma has been investigated as an inorganic dispersion material
for poorly soluble active pharmaceutical ingredients (API) in order to increase their
dissolution rates. The API is first dispersed in a suitable solvent such as acetone,
which is then added to AEROPERL® 300 Pharma. The acetone is then evaporated off
resulting into adsorption of the API onto the surface of the mesoporous silica.

Enzyme Encapsulation into Mesoporous Silica for Biocatalysis

Owing to their pore size, pore structure and particle morphology mesoporous silica
materials are of interest to many applications requiring enzymes to be immobilized or
supported in situ. Immobilization of enzymes can result in enhanced stability, ease
recovery and re-use, and allow the enzyme to be used in non-aqueous solvents where
the enzyme is insoluble.

AEROPERL® 300 Pharma is ideally suited as a support material due to it mechanical

and chemical stability as well as high surface area. It is also comparatively low cost
and exhibits low non-specific protein adsorption properties. This means that
adsorption of the enzyme is least likely to compromise the enzyme conformation or
activity.

Moisture Activated Dry Granulation (MADG)

MADG is an approach to granulation carried out in a high shear granulator similar to

conventional wet granulation except that the amount of water used is limited and there
is no heat-based drying step. MADG starts with the addition of small quantities of
water to a powder mix comprising the active ingredient(s), binder and other
excipients, which is then blended under high shear to achieve agglomeration. The
mesoporous silica, as the moisture absorbing excipient, is then added to the mixture to
absorb excess moisture and to ‘dry’ the granules.

AEROPERL® 300 Pharma mesoporus silica offers an innovative approach to wet

granulation processing. Studies have shown that AEROPERL® 300 Pharma serves as
an efficient moisture absorber due to its high surface area and pore volume. The added
moisture is bound effectively to create a stable, functional dry granular powder that
can be readily processed via tabletting, capsule filling or dosing into sachets.