小鼠体内半边旗5F微乳剂的药动学及组织分布特征  

Pharmacokinetics and Tissues Distribution of 5F Microemulsion in Mice after Oral Administration

作　　者：吕应年[1,2] 何宇辉[3] 田乐[2] 黄译锋[3] 李立[2] 吴科锋[2] 

机构地区：[1]华东理工大学化学系,上海200238 [2]广东医学院广东天然药物研究与开发重点实验室,广东湛江524023 [3]广东医学院药学院,广东东莞523808

出　　处：《中国实验方剂学杂志》2013年第18期164-168,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：广东省自然科学基金项目(S2012010008163);广东高校优秀青年创新人才培育项目(201012103)

摘　　要：目的:考察半边旗抗癌二萜5F口服微乳剂在小鼠体内的组织分布及药物代谢动力学。方法:采用Hypersil C18(4.6 mm×250 mm,5μm)色谱柱,流动相为甲醇-0.5%冰醋酸(55∶45),流速0.8 mL·min-1,进样20μL,柱温35℃。小鼠灌胃给药5F微乳剂与普通制剂后,在不同时间点取血及内脏器官,样品经处理后,采用反相高效液相色谱法测定血清及组织匀浆液中5F的浓度,分析其体内药物代谢动力学和组织分布。结果:小鼠半边旗5F微乳剂药动学参数分别为AUC0→t12.202μg·L-1·h-1,C max=3.434μg·L-1和T max=1.048 h,MRT0→t2.451 h,相对生物利用度为对照组616.15%。结论:半边旗5F微乳剂口服生物利用度提高,消除半衰期延长,具有一定的缓释作用。Objective： To investigate the pharmacokinetics and tissue distribution characteristics of the 5F oral microemulsion in mouse.Method： An Hypersil C 18（4.6 mm ×250 mm,5 μm） was adopted with the mobile phase of methanol and 0.5% acetic acid（55∶ 45） at the flow rate of 0.8 mL·min-1.The column room temperature was set at 35 ℃ and the injection volume was 20 μL.KM mice were orally administrated with 5F microemulsion at the dose of 20 mg·kg-1.At the setting time intervals,blood were collected from the ocular artery directly from the mice after eyeball removal;serum was immediately separated by centrifugation.The heart,liver,spleen,lungs and kidneys of each mouse was rapidly collected following blood collections,and immediately washed,wiped with filter paper,weighed and homogenized with normal saline to 10%.The serum and homogenates were extracted and then HPLC analysis.Result： The pharmacokinetics after oral administrations of 5F microemulsion were AUC 0→t 12.202 μg·L-1·h-1,C max.3.434 μg·L-1,T max 1.048 h,MRT 0→t 2.451 h.The relative bioavailability was 616.15% higher for microemulsion than that for the control.Conclusion： The average drug retention time was prolonged,and the relative bioavailability improved.5F microemulsion has sustainedrelease characteristic.

关 键 词：半边旗 二萜 口服微乳剂 药动学 组织分布 

分 类 号：R285.5[医药卫生—中药学]