Bioavailability Enhancement

:: Overview :: Poorly Soluble Drugs :: Poorly Permeable Drugs


Case Study

The Problem: A mid-sized pharmaceutical company had selected their lead compound from the drug discovery phase, which was an orally active cell cycle inhibitor. The drug was presented in a non-ionisable, highly crystalline state, which led to poor dissolution characteristics and low absorption. Initial studies had shown a significant improvement when using a nano-suspension formulation, but the overall % plasma concentrations did not reach the desired levels. Previous attempts to formulate an amorphous solid solution were unsuccessful due to the inherant physcial instability of the amorphous state, which led to rapid recrystallisation upon storage and a decrease in product efficacy.

The Answer: Using our formulation screening platform, we were able to carefully choose the optimal IntraSOLV® solid dispersion matrix system to stabilise the active ingredient in the amorphous state whilst giving optimal dissolution characteristics in a gastric fluid medium. The resulting powder in capsule formulation remained physically and chemically stable throughout accelerated stability investigations with no change in the enhanced dissolution properties seen.



The formulation presented above is currently in Phase II clinical trials.