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| 文章信息：Preparation and in vitro evaluation of macrocyclic metronidazole conjugates as an oral colon-specific delivery system, J. Incl. Phenom. Macrocycl. Chem., 2014, 78: 501-504 |
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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 查看期刊信息 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 查看基金资助信息 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 |
2楼2016-04-24 19:49:54
