文献类型：期刊文献

中文题名：辛伐他汀纳米脂质载体的制备及大鼠体内药动学

英文题名：Preparation and Pharmacokinetics of Simvastatin Nanostructured Lipid Carriers in Rats

作者：刘泽莹[1,2];沈淑慧[1];蒋世军[1];张志文[2];崔景斌[1]

机构：[1]华东理工大学药学院,上海200237;[2]中国科学院上海药物研究所,上海201203

年份：2013

卷号：44

期号：1

起止页码：46

中文期刊名：中国医药工业杂志

外文期刊名：Chinese Journal of Pharmaceuticals

收录：CSTPCD;;北大核心:【北大核心2011】；CSCD:【CSCD2013_2014】；

基金：国家重大科学研究计划项目(2009CB930304)

语种：中文

中文关键词：辛伐他汀;辛伐他汀酸;纳米脂质载体;制备;吸收;药动学

外文关键词：simvastatin; simvastatin acid; nanostructured lipid carrier; preparation; absorption; pharmacokinetics

摘要：采用乳化溶剂蒸发法制备辛伐他汀(1)纳米脂质载体(1-NLC),考察了其理化特性、在体肠吸收特性和大鼠体内药动学。结果表明,1-NLC平均粒径为(72.1±47.2)nm,包封率为(94.6±2.5)%,载药量为(5.78±0.57)%。在体肠吸收研究表明,与原药相比,1-NLC在十二指肠、空肠和回肠的吸收速率常数分别提高了0.5、1.3和0.6倍。大鼠体内药动学研究表明,与1混悬液组相比,1-NLC组的1及其活性代谢物辛伐他汀酸的口服生物利用度分别为222%和269%。
Simvastatin loaded nanostructured lipid carriers （1-NLC） were prepared by emulsification solvent evaporation technique. The physicochemical properties, in situ intestinal absorption and pharmacokinetic behavior in rats of 1-NLC were investigated. The results showed that 1-NLC was nanometer-sized particle with the mean diameter of （72.1±47.2）nm and the entrapment efficiency of 1-NLC was （94.6±2.5） % with the drug loading of （5.78±0.57） %. Compared with bulk drug suspension group, the absorption rate constant in duodenum, jejunum and ileum of 1-NLC group were increased by 50%, 130% and 60%, respectively. The results of pharmacokinetics in rats showed the oral bioavailability of simvastatin and its active metabolite, simvastatin acid, in 1-NLC group were 222 % and 269 % compared with the suspension group.