Population-based mechanistic prediction of oral drug absorption

AAPS J. 2009 Jun;11(2):225-37. doi: 10.1208/s12248-009-9099-y. Epub 2009 Apr 21.


The bioavailability of drugs from oral formulations is influenced by many physiological factors including gastrointestinal fluid composition, pH and dynamics, transit and motility, and metabolism and transport, each of which may vary with age, gender, race, food, and disease. Therefore, oral bioavailability, particularly of poorly soluble and/or poorly permeable compounds and those that are extensively metabolized, often exhibits a high degree of inter- and intra-individual variability. While several models and algorithms have been developed to predict bioavailability in an average person, efforts to accommodate intrinsic variability in the component processes are less common. An approach that incorporates such variability for human populations within a mechanistic framework is described together with examples of its application to drug and formulation development.

Publication types

  • Review

MeSH terms

  • Animals
  • Biological Availability
  • Biotransformation
  • Chemistry, Pharmaceutical
  • Forecasting
  • Humans
  • Intestinal Absorption
  • Pharmaceutical Preparations / metabolism*
  • Pharmacokinetics*
  • Population
  • Solubility


  • Pharmaceutical Preparations