In Vitro Test Methodologies for Characterizing Bioavailability Enhancing Formulations

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 address this trend, evaluating formulation approaches for increasing oral bioavailability are becoming routine early on in formulation development programs.

Most bioavailability enhancing formulations are designed to increase aqueous solubility and/or solubilized drug species. As such, complexities arise with respect to understanding the interplay between drug supersaturation and distribution into various components in gastrointestinal fluids and how that translates into improved performance.

More importantly, having the in vitro performance tools is crucial for characterizing and understanding enabled formulations in order to advance the appropriate formulation through development.
This webinar discusses several in vitro methodologies used at Lonza for the characterization of bioavailability enhancing formulations as well as criteria for selecting the right in vitro method based on compound properties and dose. Case studies for multiple low solubility compounds will be presented.