Fed-state gastric media and drug analysis techniques: Current status and points to consider

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• 作者：Fotios Baxevanis^a ; Jesse Kuiper^b ; Nikoletta Fotaki^a ; ^{n.fotaki@bath.ac.uk" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Fed state ; Gastric ; Biorelevant media ; Drug analysis ; Dissolution ; Bioavailability
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2016
• 出版时间：October 2016
• 年：2016
• 卷：107
• 期：Complete
• 页码：234-248
• 全文大小：811 K

文摘

Gastric fed state conditions can have a significant effect on drug dissolution and absorption. In vitro dissolution tests with simple aqueous media cannot usually predict drugs’ in vivo response, as several factors such as the meal content, the gastric emptying and possible interactions between food and drug formulations can affect drug’s pharmacokinetics. Good understanding of the effect of the in vivo fed gastric conditions on the drug is essential for the development of biorelevant dissolution media simulating the gastric environment after the administration of the standard high fat meal proposed by the FDA and the EMA in bioavailability/bioequivalence (BA/BE) studies. The analysis of drugs in fed state media can be quite challenging as most analytical protocols currently employed are time consuming and labour intensive. In this review, an overview of the in vivo gastric conditions and the biorelevant media used for their in vitro simulation are described. Furthermore an analysis of the physicochemical properties of the drugs and the formulations related to food effect is given. In terms of drug analysis, the protocols currently used for the fed state media sample treatment and analysis and the analytical challenges and needs emerging for more efficient and time saving techniques for a broad spectrum of compounds are being discussed.