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      Food, gastrointestinal pH, and models of oral drug absorption.

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          Abstract

          This article reviews the major physiological and physicochemical principles of the effect of food and gastrointestinal (GI) pH on the absorption and bioavailability of oral drugs, and the various absorption models that are used to describe/predict oral drug absorption. The rate and extent of oral drug absorption is determined by a complex interaction between a drug's physicochemical properties, GI physiologic factors, and the nature of the formulation administered. GI pH is an important factor that can markedly affect oral drug absorption and bioavailability as it may have significant influence on drug dissolution & solubility, drug release, drug stability, and intestinal permeability. Different regions of the GI tract have different drug absorptive properties. Thus, the transit time in each GI region and its variability between subjects may contribute to the variability in the rate and/or extent of drug absorption. Food-drug interactions can result in delayed, decreased, increased, and sometimes un-altered drug absorption. Food effects on oral absorption can be achieved by direct and indirect mechanisms. Various models have been proposed to describe oral absorption ranging from empirical models to the more sophisticated "mechanism-based" models. Through understanding of the physicochemical and physiological rate-limiting factors affecting oral absorption, modellers can implement simplified population-based modelling approaches that are less complex than whole-body physiologically-based models but still capture the essential elements in a physiological way and hence will be more suited for population modelling of large clinical data sets. It will also help formulation scientists to better predict formulation performance and to develop formulations that maximize oral bioavailability.

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          Author and article information

          Journal
          Eur J Pharm Biopharm
          European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
          Elsevier BV
          1873-3441
          0939-6411
          Mar 2017
          : 112
          Affiliations
          [1 ] Australian Centre for Pharmacometrics and Sansom Institute, School of Pharmacy and Medical Sciences, University of South Australia, South Australia, Australia. Electronic address: Ahmad.Abuhelwa@mymail.unisa.edu.au.
          [2 ] Australian Centre for Pharmacometrics and Sansom Institute, School of Pharmacy and Medical Sciences, University of South Australia, South Australia, Australia. Electronic address: Des.Williams@unisa.edu.au.
          [3 ] Australian Centre for Pharmacometrics and Sansom Institute, School of Pharmacy and Medical Sciences, University of South Australia, South Australia, Australia. Electronic address: Richard.Upton@unisa.edu.au.
          [4 ] Australian Centre for Pharmacometrics and Sansom Institute, School of Pharmacy and Medical Sciences, University of South Australia, South Australia, Australia. Electronic address: David.Foster@unisa.edu.au.
          Article
          S0939-6411(16)30575-6
          10.1016/j.ejpb.2016.11.034
          27914234
          471aa546-9c1c-4dc2-b887-e8d0e5f9bdcb
          History

          Gastrointestinal pH,Food-drug interactions,Empirical absorption models,Predicting oral absorption,Physiologically-based pharmacokinetic (PBPK) models

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