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Formulation of Phytosome^®

Phytosome^® complexes can be formulated both orally and topically. In order to obtain the best performances of this technogical innovation both in terms of formulating manageability and enhanced bioavailability (as appropriate disintegration and dissolution time of oral forms, for instance) Indena suggests the most appropriate manufacturing procedures to obtain effective formulations.

 

Soft gelatin capsules
Soft gelatin capsules represent an ideal solution to formulate Phytosome^® complexes.
The Phytosome^® complex can be dispersed in oily vehicles to obtain suspensions to be filled in soft gelatin capsules. Vegetable or semi-synthetic oils can be used to this purpose. We recommend a granulometry of 100% <200 μm to best perform capsule production.
According to Indena experience, not all the Phytosome^® complexes behave in the same way when dispersed in oily vehicles and when the oily suspension is filled in the soft gelatin capsules; for this reasons preliminary feasibility trials should be performed to select the most suitable vehicle.

Hard gelatin capsules
The Phytosome^® complex can be formulated in hard gelatin capsules as well. A direct volumetric filling process (withou precompression) can be applied, even if the apparently low density of the Phytosome^® complex seems to limit the maximum amount of powder that can be filled into a capsule (usually not more than 300 mg for a size 0 capsule). With a piston tamp capsule filling process, however, it is possible to increase the amount of powder which can be filled in a capsule, but precompression might affect the disintegration time. We recommend to carefully monitor the related parameters during product/process development. A preliminary dry granulation process is advisable define the best manufacturing process.

Tablets
Dry granulation represents the ideal manufacturing process to obtain tablets with higher unitary doses and with suitable technological and biopharmaceutical properties.
However, due to the limited flowability, potential stickiness and low apparent density of the Phytosome^® complex, a direct compression process can be applied only for low unitary doses; note that whenever a direct compression process is applied, the Phytosome^® complex should be diluted with 60-70% of excipients to optimize its technological properties and to obtain tablets with appropriate technological and biopharmaceutical characteristics.
On the other hand, wet granulation should be avoided due to the negative effect of water and heat (granulation/drying) on the stability of the phospholipid complex.

Topical dosage forms
The Phytosome^® complex can be formulated topically as well. The ideal process to incorporate the Phytosome^® complex in emulsion is to disperse the phospholipidic complex in a small amount of the lipidic phase and add it to the already created emulsion at low temperatures (not higher than 40°C).
The Phytosome^® complexes are dispersible in the main lipidic solvents employed in topical formulations.
In case of formulations containing a limited amount of lipids, the Phytosome^® complex might also by dispersed into the watery phase, and again added to the final formulation at temperature lower than 40°C.

 

Download the Phytosome^® formulation advises.