Drug Absorption Studies

Volume VII of the series Biotechnology: Pharmaceutical Aspects pp 182-215

In Vitro Screening Models to Assess Intestinal Drug Absorption and Metabolism

  • Sven Deferme
  • , Pieter Annaert
  • , Patrick Augustijns

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Compounds intended for oral administration must have adequate biopharmaceutical properties in order to achieve therapeutic concentrations at the targeted site of action. Different models have been established for the parallel screening of these biopharmaceutical properties, including membrane-based models (PAMPA), cell culture-based models (such as Caco-2 and MDCK cell lines), and the Ussing chambers technique. In this chapter, the strengths and the drawbacks of these models are discussed, while examples of applications for these different models and suggestions to improve the models are provided. Finally, different in vitro methods for studying the intestinal metabolism are also described. As the intestinal absorption process depends on a multitude of parameters, a single universal model accounting for all these parameters does not exist. Therefore, combination of different in vitro models should be considered in order to obtain better insights in intestinal drug absorption in the different phases of drug discovery and development.


Intestinal drug absorption Intestinal metabolism Cell culture-based models Membrane-based models Ex vivo models