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双层片剂的研制及地西泮的口腔给药特性:设计、优化与评价。

Development and characterization of bilayered tablets of diazepam for oral drug delivery: design, optimization and evaluation.

机构信息

Cardiovascular Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.

Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.

出版信息

Ther Deliv. 2022 Apr;13(4):221-231. doi: 10.4155/tde-2021-0077. Epub 2022 Mar 21.

Abstract

The oral bioavailability of drugs can be limited by their short residence time in the gastrointestinal tract. This study was performed to design bilayered floating tablets of diazepam comprising immediate-release and controlled-release layers. The tablets were prepared using sodium starch glycolate, polyvinyl pyrrolidone, hydroxypropyl methylcellulose and microcrystalline cellulose and evaluated for their characteristics. The optimized formulation was found to be buoyant for 8 h on simulated gastric fluid. Hydroxypropyl methylcellulose K4M and microcrystalline cellulose sustained the release of diazepam from the controlled-release layer. The optimized formulation exhibited an extended release period of 8 h. It can be concluded that bilayered tablets of diazepam may extend the residence time of the drug at the site of absorption.

摘要

药物的口服生物利用度可能会受到其在胃肠道中停留时间短的限制。本研究旨在设计包含速释和缓释层的地西泮双层漂浮片剂。这些片剂采用交联羧甲基淀粉钠、聚乙烯吡咯烷酮、羟丙甲纤维素和微晶纤维素制备,并对其特性进行了评估。优化的配方在模拟胃液中具有 8 小时的漂浮能力。羟丙甲纤维素 K4M 和微晶纤维素使地西泮从缓释层中持续释放。优化的配方表现出 8 小时的延长释放期。可以得出结论,地西泮双层片剂可以延长药物在吸收部位的停留时间。

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