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【答案】应助回帖
★ ★ ★ ★ ★
感谢参与，应助指数 +1
wangzzsc: 金币+5, ★★★★★最佳答案, 十分感谢！ 2016-04-24 19:53:05
心静_依然: LS-EPI+1, 感谢应助 2016-04-24 22:05:17
OURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY
卷: 78 期: 1-4 页: 501-504
DOI: 10.1007/s10847-013-0339-5
出版年: APR 2014
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摘要
The antimicrobial drug metronidazole (MTZ) was covalently conjugated to the secondary hydroxyl groups of beta-cyclodextrin through ester linkage using sodium hydride as the deproton reagent. The preliminary release behavior of MTZ in rat gastrointestinal tract contents was studied at 37 degrees C within 24 h. In the contents of stomach, the conjugates did hardly release MTZ, released MTZ only 9.5 % in the contents of small intestine, and released MTZ significantly up to 43.6 and 40.2 % in the contents of cecum and colon, respectively. These results indicate that the conjugate activation took place site-specifically in the rat cecal and colonic contents, probably via the biodegradation by glycosidases and hydrolases. The present MTZ-appended cyclodextrin conjugate may be of value as an orally administered delayed-release and/or colon-specific prodrug.
关键词
作者关键词:beta-Cyclodextrin; Conjugate; Colon-specific delivery; Metronidazole; Prodrug
KeyWords Plus:ENZYMATIC-HYDROLYSIS; DRUG-DELIVERY; CYCLODEXTRINS; PRODRUGS
作者信息
通讯作者地址: Wei, SJ (通讯作者)
显示增强组织信息的名称 Ningxia Med Univ, Gen Hosp, Dept Pharm, Yinchuan 750004, Peoples R China.
地址:
显示增强组织信息的名称 [ 1 ] Ningxia Med Univ, Gen Hosp, Dept Pharm, Yinchuan 750004, Peoples R China
电子邮件地址:weisjnx@163.com
基金资助致谢
基金资助机构 授权号
Ningxia's Natural Science Foundation
NZ12178
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出版商
SPRINGER, VAN GODEWIJCKSTRAAT 30, 3311 GZ DORDRECHT, NETHERLANDS
类别 / 分类
研究方向:Chemistry
Web of Science 类别:Chemistry, Multidisciplinary
文献信息
文献类型:Article
语种:English
入藏号: WOS:000334496700049
ISSN: 0923-0750
eISSN: 1573-1111
期刊信息
Impact Factor (影响因子): Journal Citation Reports®
其他信息
IDS 号: AF1TM
Web of Science 核心合集中的 "引用的参考文献": 16
Web of Science 核心合集中的 "被引频次": 2 |
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