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Review

Food Effects on Oral Drug Absorption: Application of Physiologically-Based Pharmacokinetic Modeling as a Predictive Tool

Faculty of Pharmaceutical Sciences, The University of British Columbia, Vancouver, BC V6T 1Z3, Canada
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Pharmaceutics 2020, 12(7), 672; https://doi.org/10.3390/pharmaceutics12070672
Received: 21 June 2020 / Revised: 15 July 2020 / Accepted: 15 July 2020 / Published: 17 July 2020
(This article belongs to the Special Issue Mechanistic In Vitro and In Silico Modeling of Oral Drug Absorption)
The bioavailability of an orally administered small molecule is often dictated by drug-specific physicochemical characteristics and is influenced by many biological processes. For example, in fed or fasted conditions, the transit time within the gastrointestinal tract can vary, confounding the ability to predict the oral absorption. As such, the effects of food on the pharmacokinetics of compounds in the various biopharmaceutics classification system (BCS) classes need to be assessed. The consumption of food leads to physiological changes, including fluctuations in the gastric and intestinal pH, a delay in gastric emptying, an increased bile secretion, and an increased splanchnic and hepatic blood flow. Despite the significant impact of a drug’s absorption and dissolution, food effects have not been fully studied and are often overlooked. Physiologically-based pharmacokinetic (PBPK) models can be used to mechanistically simulate a compound’s pharmacokinetics under fed or fasted conditions, while integrating drug properties such as solubility and permeability. This review discusses the PBPK models published in the literature predicting the food effects, the models’ strengths and shortcomings, as well as future steps to mitigate the current knowledge gap. We observed gaps in knowledge which limits the ability of PBPK models to predict the negative food effects and food effects in the pediatric population. Overall, the further development of PBPK models to predict food effects will provide a mechanistic basis to understand a drug’s behavior in fed and fasted conditions, and will help enable the drug development process. View Full-Text
Keywords: food effects; physiologically-based pharmacokinetic model; oral absorption; mathematical modeling food effects; physiologically-based pharmacokinetic model; oral absorption; mathematical modeling
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MDPI and ACS Style

Cheng, L.; Wong, H. Food Effects on Oral Drug Absorption: Application of Physiologically-Based Pharmacokinetic Modeling as a Predictive Tool. Pharmaceutics 2020, 12, 672. https://doi.org/10.3390/pharmaceutics12070672

AMA Style

Cheng L, Wong H. Food Effects on Oral Drug Absorption: Application of Physiologically-Based Pharmacokinetic Modeling as a Predictive Tool. Pharmaceutics. 2020; 12(7):672. https://doi.org/10.3390/pharmaceutics12070672

Chicago/Turabian Style

Cheng, Lisa, and Harvey Wong. 2020. "Food Effects on Oral Drug Absorption: Application of Physiologically-Based Pharmacokinetic Modeling as a Predictive Tool" Pharmaceutics 12, no. 7: 672. https://doi.org/10.3390/pharmaceutics12070672

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