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Physiological Considerations and In Vitro Strategies for Evaluating the Influence of Food on Drug Release from Extended-Release Formulations

  • Review Article
  • Theme: Advancements in Dissolution Testing of Oral and Non-Oral Formulations
  • Published:
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Abstract

Food effects on oral drug bioavailability are a consequence of the complex interplay between drug, formulation and human gastrointestinal (GI) physiology. Accordingly, the prediction of the direction and the extent of food effects is often difficult. With respect to novel formulations, biorelevant in vitro methods can be extremely powerful tools to simulate the effect of food-induced changes on the physiological GI conditions on drug release and absorption. However, the selection of suitable in vitro methods should be based on a thorough understanding not only of human GI physiology but also of the drug and formulation properties. This review focuses on in vitro methods that can be applied to evaluate the effect of food intake on drug release from extended release (ER) products during preclinical formulation development. With the aid of different examples, it will be demonstrated that the combined and targeted use of various biorelevant in vitro methods can be extremely useful for understanding drug release from ER products in the fed state and to be able to forecast formulation-associated risks such as dose dumping in early stages of formulation development.

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Authors and Affiliations

  1. Department of Biopharmaceutics and Pharmaceutical Technology, University of Greifswald, Center of Drug Absorption and Transport, Felix-Hausdorff-Str. 3, 17487, Greifswald, Germany

    Mirko Koziolek

  2. Institute of Pharmaceutical Technology, Goethe University, Max-von-Laue-Str. 9, 60438, Frankfurt am Main, Germany

    Edmund Kostewicz

  3. Department of Pharmacy, School of Health Science, National and Kapodistrian University of Athens, Panepistimiopolis, 157 84, Athens, Greece

    Maria Vertzoni

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  1. Mirko Koziolek
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  2. Edmund Kostewicz
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Correspondence to Mirko Koziolek.

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Koziolek, M., Kostewicz, E. & Vertzoni, M. Physiological Considerations and In Vitro Strategies for Evaluating the Influence of Food on Drug Release from Extended-Release Formulations. AAPS PharmSciTech 19, 2885–2897 (2018). https://doi.org/10.1208/s12249-018-1159-0

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