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

AAPS PharmSciTech
Mirko KoziolekMaria Vertzoni

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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Citations

Apr 7, 2020·Expert Opinion on Drug Delivery·Marival BermejoIsabel Gonzalez-Alvarez
Oct 24, 2020·Pharmaceutical Research·Valentyn MohylyukAndriy Dashevskiy
Feb 17, 2021·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Leonardo Antonio PintoJosé Ricardo de Arruda Miranda
Mar 14, 2021·Journal of the Science of Food and Agriculture·Juan HanGuo-Peng Miao

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Methods Mentioned

BETA
pharmacotherapy
in vitro methods

Software Mentioned

Simcyp®
PK
OROS
Sim®
StressTest
TNO TIM -
SmartPill
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