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新型黄酮类衍生物DA-6034用于治疗胃炎的胃滞留给药系统

Gastroretentive drug delivery system of DA-6034, a new flavonoid derivative, for the treatment of gastritis.

作者信息

Jang Sun Woo, Lee Jung Woo, Park Sung Hyun, Kim Jeong Hoon, Yoo Moohi, Na Dong Hee, Lee Kang Choon

机构信息

Research Laboratory, Dong-A Pharmaceutical Company, 47-5 Sanggal-dong, Kiheung-ku, Yongin 446-905, South Korea.

出版信息

Int J Pharm. 2008 May 22;356(1-2):88-94. doi: 10.1016/j.ijpharm.2007.12.042. Epub 2008 Jan 9.

Abstract

A gastroretentive drug delivery system of DA-6034, a new synthetic flavonoid derivative, for the treatment of gastritis was developed by using effervescent floating matrix system (EFMS). The therapeutic limitations of DA-6034 caused by its low solubility in acidic conditions were overcome by using the EFMS, which was designed to cause tablets to float in gastric fluid and release the drug continuously. The release of DA-6034 from tablets in acidic media was significantly improved by using EFMS, which is attributed to the effect of the solubilizers and the alkalizing agent such as sodium bicarbonate used as gas generating agent. DA-6034 EFMS tablets showed enhanced gastroprotective effects in gastric ulcer-induced beagle dogs, indicating the therapeutic potential of EFMS tablets for the treatment of gastritis.

摘要

通过使用泡腾漂浮基质系统(EFMS)开发了一种用于治疗胃炎的新型合成黄酮衍生物DA-6034的胃滞留药物递送系统。通过使用EFMS克服了DA-6034在酸性条件下低溶解度所导致的治疗局限性,该系统旨在使片剂漂浮在胃液中并持续释放药物。使用EFMS显著改善了酸性介质中片剂中DA-6034的释放,这归因于增溶剂和用作产气剂的碱化剂(如碳酸氢钠)的作用。DA-6034 EFMS片剂在胃溃疡诱导的比格犬中显示出增强的胃保护作用,表明EFMS片剂在治疗胃炎方面的治疗潜力。

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