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环丙沙星漂浮型生物黏附缓释片的制剂与体外特性研究

Formulation and in vitro characterization of ciprofloxacin floating and bioadhesive extended-release tablets.

作者信息

Varshosaz Jaleh, Tavakoli N, Roozbahani F

机构信息

Department of Pharmaceutics, School of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

Drug Deliv. 2006 Jul-Aug;13(4):277-85. doi: 10.1080/10717540500395106.

Abstract

Ciprofloxacin is mainly absorbed in the proximal areas of the gastrointestinal tract. The purpose of our study was production of floating-bioadhesive tablets to lengthen the stay of drug in its absorption area. Effervescent tablets were made using sodium carboxymethyl cellulose (CMC), hydroxypropyl methylcellulose (HPMC), polyacrylic acid (AA), polymetacrylic acid (MAA), citric acid, and sodium bicarbonate. Tablets with 5% effervescent base had longer lag time than 10%. The type of polymer had no significant effect on the floating lag time. All tablets floated atop the medium for 23-24 hr. Increasing CMC caused higher mucoadhesion than AA (p < 0.05). All formulations showed a Higuchi, non-Fickian release mechanism. Tablets with 10% effervescent base, 80% CMC/20% HPMC, or 80% AA /20% MAA seemed desirable.

摘要

环丙沙星主要在胃肠道近端吸收。我们研究的目的是制备胃内漂浮生物黏附片,以延长药物在其吸收部位的停留时间。泡腾片采用羧甲基纤维素钠(CMC)、羟丙基甲基纤维素(HPMC)、聚丙烯酸(AA)、聚甲基丙烯酸(MAA)、柠檬酸和碳酸氢钠制成。含5%泡腾碱的片剂比含10%泡腾碱的片剂滞后时间更长。聚合物类型对漂浮滞后时间无显著影响。所有片剂在介质表面漂浮23 - 24小时。增加CMC比增加AA导致更高的黏膜黏附性(p < 0.05)。所有制剂均呈现 Higuchi 非 Fick 扩散释放机制。含10%泡腾碱、80% CMC/20% HPMC或80% AA /20% MAA的片剂似乎较为理想。

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