Navigating the human gastrointestinal tract for oral drug delivery: Uncharted waters and new frontiers

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• 作者：Mirko Koziolek^a ; ^b ; Michael Grimm^a ; Felix Schneider^a ; Philipp Jedamzik^a ; Maximilian Sager^a ; Jens-Peter Kü ; hn^c ; Werner Siegmund^d ; Werner Weitschies^a ; ^{werner.weitschies@uni-greifswald.de" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Drug absorption ; Oral drug delivery ; Gastrointestinal dynamics ; Gastrointestinal hydrodynamics ; Gastrointestinal motility ; Absorption window ; Food effect ; Biorelevant dissolution testing
• 刊名：Advanced Drug Delivery Reviews
• 出版年：2016
• 出版时间：1 June 2016
• 年：2016
• 卷：101
• 期：Complete
• 页码：75-88
• 全文大小：1872 K

文摘

Many concepts of oral drug delivery are based on our comprehension of human gastrointestinal physiology. Unfortunately, we tend to oversimplify the complex interplay between the various physiological factors in the human gut and, in particular, the dynamics of these transit conditions to which oral dosage forms are exposed. Recent advances in spatial and temporal resolution of medical instrumentation as well as improved access to these technologies have facilitated clinical trials to characterize the dynamic processes within the human gastrointestinal tract. These studies have shown that highly relevant parameters such as fluid volumes, dosage form movement, and pH values in the lumen of the upper GI tract are very dynamic. As a result of these new insights into the human gastrointestinal environment, some common concepts and ideas of oral drug delivery are no longer valid and have to be reviewed in order to ensure efficacy and safety of oral drug therapy.