Material-Sparing Formulation Strategies for Enhancing Bioavailability of Challenging Beyond Rule of Five (bRo5) Molecules
Summary: Formulating Beyond Rule of Five (bRo5) molecules presents significant bioavailability and development challenges, especially for small or emerging pharma with limited API and constrained budgets. In this case study, discover how Catalent partnered with a small pharmaceutical company to overcome solubility and permeability hurdles for a DCS IIb compound using a material-sparing strategy. Through mechanistic in vitro membrane flux testing, biorelevant micelle systems, and scalable lipid-based and amorphous solid dispersion (ASD) prototypes, Catalent enabled a 3x increase in Cmax in vivo. This case illustrates Catalent’s ability to rapidly advance challenging molecules with minimal API and accelerate early-stage development through science-driven, bioavailability-enhancing formulation approaches.