In vivo methods for drug absorption - comparative physiologies, model selection, correlations with in vitro methods (IVIVC), and applications for formulation/API/excipient characterization including food effects

Eur J Pharm Sci. 2014 Jun 16;57:99-151. doi: 10.1016/j.ejps.2014.02.010. Epub 2014 Mar 15.


This review summarizes the current knowledge on anatomy and physiology of the human gastrointestinal tract in comparison with that of common laboratory animals (dog, pig, rat and mouse) with emphasis on in vivo methods for testing and prediction of oral dosage form performance. A wide range of factors and methods are considered in addition, such as imaging methods, perfusion models, models for predicting segmental/regional absorption, in vitro in vivo correlations as well as models to investigate the effects of excipients and the role of food on drug absorption. One goal of the authors was to clearly identify the gaps in today's knowledge in order to stimulate further work on refining the existing in vivo models and demonstrate their usefulness in drug formulation and product performance testing.

Keywords: Bioavailability; Biopharmaceutic characterization; Drug product development; In vivo model selection.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Biopharmaceutics / methods*
  • Chemistry, Pharmaceutical
  • Excipients / chemistry*
  • Food-Drug Interactions*
  • Gastrointestinal Motility
  • Gastrointestinal Tract / metabolism*
  • Humans
  • Intestinal Absorption*
  • Models, Animal
  • Models, Biological
  • Pharmaceutical Preparations / administration & dosage
  • Pharmaceutical Preparations / chemistry
  • Pharmaceutical Preparations / metabolism*
  • Pharmacokinetics*
  • Reproducibility of Results
  • Species Specificity


  • Excipients
  • Pharmaceutical Preparations