Most new drug candidates suffer from poor water- solubility leading to rate limiting dissolution, slow absorption and limited bioavailability. Solid amorphous drug dispersions are most commonly used improve bioavailability by enhancing drug solubility. The selection of the right solid dispersion formulation not only requires a thorough understanding of the API itself, but also an extensive knowledge of excipients and solid dispersion technologies.Controlled release of poorly water-soluble drugs is yet another challenge for formulators. Solid dispersions generally tend to be immediate-release forms with the inherent drawbacks of high peak drug concentrations in the blood as well as relatively short durations of effective concentration levels in the blood. The combined and synergistic approaches of controlled release and solid dispersions containing poorly water-soluble drugs have become a valuable technique to achieve optimal drug bioavailability in a controlled manner and thereby providing the predictability and reproducibility of the drug release kinetics.In this presentation, several case studies will be used to review the rational design of solid dispersion formulations including commonly employed approaches, excipient selection and process technologies. Additionally, a new hot melt extrusion formulation platform for controlled release of poorly water-soluble drugs would be highlighted.
Program Manager - Global Pharmaceutical R&D and Technical Services RoA