Amorphous Solid Dispersions: Utilization and Challenges in Drug Discovery and Development

摘要: Amorphous solid dispersion (ASD) can accelerate a project by improving dissolution rate and solubility, offering dose escalation flexibility excipient acceptance for toxicology studies, as well providing adequate preclinical clinical exposure. The prerequisite physicochemical properties compound to form stable ASD are glass-forming ability low-crystallization tendency, which be assessed using computational tools experimental methods. Polymer screening in silico miscibility prediction techniques is discussed. Improved technologies polymer with minimal quantity of drug substance, the scalability from bench commercial reviewed. Considerations vitro evaluations, animal selection, translation results studies also Better understanding how polymers improve stability amorphous phase state improves bioavailability have facilitated applications ranging discovery research development further commercialization. With ASDs currently used pharmaceutical industry what challenges remain solved, applied solve formulation problems at given stages. © 2015 Wiley Periodicals, Inc. American Pharmacists Association J Pharm Sci 104:3237–3258,