This presentation details a case study on the development of a generic equivalent for Intelence (Etravirine), a poorly soluble drug, utilizing KinetiSol® amorphous dispersion technology. We will walk through the process of creating a predictive in-vitro dissolution method using MacroFLUX by first establishing a correlation with canine pharmacokinetic (PK) data and subsequently continuing to update it against human PK results. This robust model guided formulation modifications, specifically adjusting the sodium stearyl fumarate (SSF) concentration, which proved critical to matching the reference product's performance in both fed and fasted human PK studies. The success of this approach highlights the utility of employing a predictive tool like MacroFLUX to de-risk development and efficiently guide formulation strategies for challenging compounds, demonstrating its value in accurately forecasting human outcomes as development continues. Retroactively the predictor tool was utilized to estimate a fraction absorbed value based on the in-vitro data and compared to the in-vivo data.
