辛伐他汀纳米脂质载体的制备及大鼠体内药动学  

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] 

机构地区：[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

出　　处：《中国医药工业杂志》2013年第1期46-49,共4页Chinese Journal of Pharmaceuticals

基　　金：国家重大科学研究计划项目(2009CB930304)

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.

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 

分 类 号：R944.9[医药卫生—药剂学]