多烯紫杉醇脂质体大鼠体内药物动力学研究  

Pharmacokinetics Study on Docetaxel Liposome in Rats

作　　者：刘睿颖[1] 王盛民[1] 宋庆国 

机构地区：[1]西南交通大学药学院,四川峨眉山614202 [2]科瑞德·凯华制药有限公司,四川成都610041

出　　处：《时珍国医国药》2009年第1期56-57,共2页Lishizhen Medicine and Materia Medica Research

基　　金：四川省中医药管理局资助课题(No.2006-72)

摘　　要：目的探讨多烯紫杉醇脂质体大鼠体内代谢过程。方法优化色谱条件，以萃取浓集法处理生物样品，内标法测定样品中药物含量；SD大鼠尾静脉给药后测定设定时间点体内药物浓度，用2．0版DAS软件分析药物体内动力学参数。结果经优化色谱条件，在0．05～25μg／ml浓度范围内，多烯紫杉醇线性关系良好。药物体内过程符合双室模型，主要药物代谢动力学参数均值为：分布半衰期（T1/2α）为2．374min；消除半衰期（T1/2β）为299．038min；清除率（CL）为0．026L/（min·mg）；表观分布容积（V1）为0．219L/kg。结论该研究为开发多烯紫杉醇脂质体提供体内动力学参考。Objective To establish an HPLC method for in vivio docetaxel determination and do some research on pharmacokinetics of docetaxel liposomes in rats. Methods HPLC method was optimized and samples were concentrated via ether extraction and determined with inner - standard method. Docetaxel liposome was given intravenously at 10 mg/kg to SD rats and blood sample was taken at chosen time interval and docetaxel conentration was determined, according to which pharmacokinetic parameters were gained via DAS 2.0. Results The chosen mobile phase was methonol： water（45： 55） and wavelength was 233nm. Within the range of 0.05～ 25μg/ml there was an excellent linear correlation and the regression equation of peak area ratio to concentration was Y = 0. 396 8 X ＋ 0.680 8 （ r = 0. 999 4）. The pharmacokinetic result revealed it a double - department model and the kinetic parameters were T1/2 a = 2. 374min, T1/2 β = 299. 038 min, CL = 0. 026 L/（ min mg） and V1 = 0. 219 L/kg. Conclusion The study focused on kinetic properties of docetaxel liposome in order to provide theoratical support for clinical researches.

关 键 词：多烯紫杉醇 脂质体 药物代谢动力学 大鼠 

分 类 号：R962[医药卫生—药理学]