Pharmaceutical Research

, 35:55 | Cite as

Lipids in the Stomach – Implications for the Evaluation of Food Effects on Oral Drug Absorption

  • Mirko Koziolek
  • Frédéric Carrière
  • Christopher J. H. Porter
Expert Review


Food effects on oral drug bioavailability can have significant impact on the provision of safe and reliable oral pharmacotherapy. A mechanistic understanding of the events that contribute to the occurrence of food effects is therefore critical. An increased oral bioavailability is often seen for poorly water-soluble drugs after co-administration with lipids, including lipids in food, and is commonly explained by the ability of lipids to enhance drug solubility in intestinal luminal fluids. In contrast, the impact of lipids on drug solubilisation in the stomach has received less attention. This is in spite of the fact that lipid digestion is initiated in the stomach by human gastric lipase and that gastric events also initiate emulsification of lipids in the gastrointestinal tract. The stomach therefore acts to ‘pre-process’ lipids for subsequent events in the intestine and may significantly affect downstream events at intestinal drug absorption sites. In this article, the mechanisms by which lipids are processed in the stomach are reviewed and the potential impact of these processes on drug absorption discussed. Attention is also focused on in vitro methods that are used to assess gastric processing of lipids and their application to better understand food effects on drug release and absorption.


Biorelevant dissolution Food effect Gastric lipolysis Human gastric lipase In vitro digestion Lipids Milk 



Area under the curve






Dog Gastric Lipase


European Medicines Agency


United States Food and Drug Administration


Free Fatty acid


Human Gastric Fluid


Human Gastric Lipase


Lipid Based Formulations


Long chain fatty acid


Long chain triacylglycerol


Lipid Formulation Classification System




Medium chain fatty acid


Medium chain triacylglycerol


Magnetic resonance imaging


Pancreatic exocrine insufficiency


Poorly water-soluble drugs


Recombinant Dog Gastric Lipase


Rabbit Gastric Extract


Simulated Gastric Fluid




Short chain fatty acid



This work was supported by a fellowship within the Postdoc-Program of the German Academic Exchange Service (DAAD).


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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  • Mirko Koziolek
    • 1
    • 2
  • Frédéric Carrière
    • 3
  • Christopher J. H. Porter
    • 2
    • 4
  1. 1.Department of Biopharmacy and Pharmaceutical Technology, Center of Drug Absorption and TransportUniversity of Greifswald, GermanyGreifswaldGermany
  2. 2.Drug Delivery Disposition and Dynamics, Monash Institute of Pharmaceutical SciencesMonash UniversityParkvilleAustralia
  3. 3.Aix-Marseille Université, CNRS, UMR 7282 Enzymologie Interfaciale et de Physiologie de la LipolyseMarseille Cedex 20France
  4. 4.ARC Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical SciencesMonash UniversityParkvilleAustralia

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