Formulating Amorphous Solid Dispersions: Key Challenges and Considerations for a Streamlined Approach

3/16/2021 15:30 - 16:05

A large and increasing fraction of orally administered small molecules in pharma company pipelines have poor oral absorption due to low aqueous solubility or dissolution rate. To overcome these limitations, formulation approaches for increasing oral bioavailability are needed. Amorphous solid dispersions (ASDs) are a prevalent technology for addressing oral bioavailability challenges, given the applicability and scalability of the technology across a diverse compound physicochemical space. Developing ASDs requires an integrated approach, where bioperformance, physical and chemical stability as well as manufacturability are all considered. Combining knowledge of key drug, polymer and gastrointestinal properties together with an in vitro and in silico toolkit is critical for achieving optimal in vivo performance while reducing development timelines and drug substance requirements. This presentation covers some general strategies for developing a successful amorphous solid dispersion formulation, from formulation intermediates to final dosage forms.

Aaron Stewart, Associate Principal Scientist, Lonza