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综述文章:延迟释放质子泵抑制剂制剂之间的异同

Review article: similarities and differences among delayed-release proton-pump inhibitor formulations.

作者信息

Horn J R, Howden C W

机构信息

Department of Pharmacy, University of Washington, Seattle, WA, USA.

出版信息

Aliment Pharmacol Ther. 2005 Dec;22 Suppl 3:20-4. doi: 10.1111/j.1365-2036.2005.02714.x.

Abstract

Proton-pump inhibitors are acid-labile, and require an enteric coating to protect them from degradation in the stomach when given orally. However, this leads to delayed absorption and onset of action of the proton-pump inhibitor. This article aims to review the similarities and differences between the various formulations of delayed release proton-pump inhibitors. Delayed-release omeprazole and delayed-release lansoprazole have been suspended in sodium bicarbonate for tube administration; however, for omeprazole, absorption is further impaired and antisecretory effects are disappointing. Although such formulations may be more convenient for clinical use in certain patient groups, absorption of the proton-pump inhibitor is still influenced by residual enteric coating. There are few differences among the currently available delayed-release proton-pump inhibitors with respect to their pharmacodynamic effects during chronic administration. There are minor formulation-based pharmacokinetic differences among these agents, primarily reflected in their bioavailability following the first few doses. Differences in bioavailability may explain slight differences in the rate of onset of maximal antisecretory effect. However, minor pharmacodynamic and pharmacokinetic differences are not associated with meaningful differences in clinical outcomes.

摘要

质子泵抑制剂对酸不稳定,口服时需要肠溶包衣以保护其在胃中不被降解。然而,这会导致质子泵抑制剂的吸收延迟和起效延迟。本文旨在综述不同剂型的缓释质子泵抑制剂之间的异同。缓释奥美拉唑和缓释兰索拉唑已被悬浮于碳酸氢钠中用于管饲;然而,对于奥美拉唑,吸收会进一步受损,抑酸效果也不尽人意。尽管此类剂型在某些患者群体中临床使用可能更方便,但质子泵抑制剂的吸收仍受残留肠溶包衣的影响。目前可用的缓释质子泵抑制剂在长期给药期间的药效学效应方面差异不大。这些药物之间存在基于剂型的微小药代动力学差异,主要体现在最初几次给药后的生物利用度上。生物利用度的差异可能解释最大抑酸效应起效速率的细微差异。然而,微小的药效学和药代动力学差异与临床结局的有意义差异无关。

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