In Vitro and In Vivo Assessment of the Potential of Supersaturation to Enhance the Absorption of Poorly Soluble Basic Drugs

Purpose Delaying precipitation of weakly basic drugs in supersaturated state following their transition from the acidic gastric environment to the near-neutral proximal small intestinal fluid is emerging as a promising tactic for achieving higher transitional solubility and improving bioavailability of such drugs. The aim of this study was to assess the effect of supersaturation on drug dissolution and permeation in vitro, and to evaluate the in vitro-in vivo correlation of the supersaturation effect for the poorly soluble basic drug ketoconazole.