Quantitation of small intestinal permeability during normal human drug absorption.

ABSTRACT:

Background

Understanding the quantitative relationship between a drug's physical chemical properties and its rate of intestinal absorption (QSAR) is critical for selecting candidate drugs. Because of limited experimental human small intestinal permeability data, approximate surrogates such as the fraction absorbed or Caco-2 permeability are used, both of which have limitations.

Methods

Given the blood concentration following an oral and intravenous dose, the time course of intestinal absorption in humans was determined by deconvolution and related to the intestinal permeability by the use of a new 3 parameter model function ("Averaged Model" (AM)). The theoretical validity of this AM model was evaluated by comparing it to the standard diffusion-convection model (DC). This an

SUBMITTER: Levitt DG 

PROVIDER: S-EPMC3734790 | biostudies-literature | 2013 Jun

REPOSITORIES: biostudies-literature