Small Molecule Formulation Screening Strategies in Drug Discovery

The correct formulation of new drug candidate compounds in drug discovery is mandatory since the majority of go/no-go decisions to advance candidates are based on in vitro ADME, receptor binding, in vivo pharmacokinetic and efficacy screens. For this reason, having a rapid formulation screen would be a valuable tool for chemists and biologists working in drug discovery. This chapter will describe a rapid solubilization screen that consumes minimal amounts of compound using an HPLC detection method to measure the solubility of drug candidates in various formulations. Using the pKa and Log P of the compound, formulation selection for drug candidates are based on a decision tree approach to guide the user in the selection of appropriate formulations.