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

Yuri Bukhtiyarov, Jibin Li, Nicole Spivey, Svitlana Silchenko, Christopher Force, Carlos Hidalgo, Yuehua Huang, Albert J. Owen, Ismael J. Hidalgo
Absorption Systems, LLC

This poster was presented at AAPS PharmSci 360, 2019

Inducing supersaturation is an attractive approach for increasing the systemic absorption of poorly soluble drugs. Delayed 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 improved bioavailability of such drugs. The purpose of this study was to assess the effect of pH-shift induced supersaturation on drug dissolution and permeation in vitro, and to evaluate the approach of extending supersaturation to enhance drug oral absorption in vivo.