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Formulation of Phytosome®

Phytosome® 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 optimized 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®. A Phytosome® 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® formnulations 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® 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® 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® formulation, a direct compression process can be applied only for low unitary doses; note that whenever a direct compression process is applied, the Phytosome® 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 formulation.