In Silico Modeling of Non-Linear Drug Absorption for the P-gp Substrate Talinolol and of Consequences for the Resulting Pharmacodynamic Effect

Authors: Tubic-Grozdanis M, Wagner D, Spahn-Langguth H, Bolger MB, Langguth P
Publication: AAPS J
Keywords: absorption, intestinal efflux, P-glycoprotein, pharmacokinetics, simulation, talinolol
Software: GastroPlus®
Division: Simulations Plus

Purpose

The aim of the present work was to demonstrate P-glycoprotein’s involvement in the non-linear talinolol pharmacokinetics using an advanced compartment and transit model (ACAT) and to compare the results predicted from the model to the finding of a phase I dose escalation study with oral talinolol doses increasing from 25 to 400 mg.

By Michael B Bolger