Hot-Melt Extrusion of Amorphous Solid Dispersions for Bioavailability Enhancement

A large majority of active pharmaceutical ingredients (API) currently in development have limited bioavailability due to low solubility and dissolution rates (BCS/DCS IIa and IIb). Bend Research, part of Capsugel Dosage Form Soultions, has a multitude of established technologies and rigorous selection criteria to address this problem on a per API basis. One approach, hot-melt extrusion (HME) of amorphous solid dispersions is a mature and commercial ready technology platform. The company uses an integrated process and formulation approach to HME that balances the target absorption profile, manufacturability, physical and chemical stability, and API availability to develop a progressable solid dispersion drug intermediate and dosage form that is robust and scalable. Strategies and case studies for solid dispersion formulation selection and definition of a HME process operating space will be reviewed.