Barbra H. Stewart

TL;DR: Prodrug strategies coupling drug solubilization with membrane carrier targeting and the use of collapsible and bifunctional prodrugs are outlined, and studies utilizing model compounds to test the strategy are illustrated.

TL;DR: These findings support absorption of gabapentin by a saturable pathway, system L, shared by the large hydrophobic amino acids, L-Phe and L-Leu, made a major contribution to the lack of proportionality in plasma levels of drug with increasing dose ob-served in the clinic.

TL;DR: The results support caution in extrapolating correlations based on findings with small organic molecules to the behavior of complex peptidomimetics, and suggest that CACO-2 cell monolayers and rat single-pass intestinal perfusion combine the highest correlation between systems, most defined relationship with fraction absorbed in humans, and experimental logistics in-line with discovery candidates.

TL;DR: This study demonstrated that atorvastatin was secreted across the apical surface of Caco-2 cell monolayers via P-glycoprotein-mediated efflux and transported across theApical membrane in theabsorptive direction via a H+-monocarboxylic acid cotransporter(MCT).

TL;DR: This review illustrates the relationships between physicochemical parameters, intestinal permeability and hepatic processing, using a set of eight peptidomimetic renin inhibitor analogs to provide suggestions for the design of compounds with improved bioavailability.