延胡索乙素在大鼠体内的立体选择性药代动力学  

Stereoselective pharmacokinetics of tetrahydropalmatine in rats

作　　者：洪战英[1] 范国荣[1] 柴逸峰[1] 闻俊[1] 殷学平[1] 吴玉田[1] 

机构地区：[1]中国人民解放军第二军医大学药学院

出　　处：《药学学报》2005年第8期746-749,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(30271603)

摘　　要：目的研究dl延胡索乙素在大鼠体内的立体选择性动力学过程。方法血浆样品经液液萃取后,用非手性手性HPLC联用法测定血浆中延胡索乙素对映体的浓度,配对t检验比较两对映体的血药浓度和药代动力学参数。结果大鼠血浆中l延胡索乙素的浓度均明显高于d延胡索乙素的浓度,两对映体的AUC,MRT和Cmax均有显著性差异。结论大鼠灌胃延胡索乙素消旋体后,两对映体在体内的药代动力学过程具有显著的立体选择性。Aim To investigate the stereoselective pharmacokinetic process of tetrahydropalmatine （THP） in rats. Methods The concentrations of tetrahydropalmatine enantiomers in rat plasma were determined by coupled achiral and chiral HPLC method. The differences in plasma concentrations and pharmacokinetic parameters between the two enantiomers were compared by paired t-test. Results The plasma levels of l-THP were always higher than those of d-THP in eight rats. There was significant difference between the main pharmacokinetic parameters of the two enantiomers. Conclusion Tetrahydropalmatine showed significant stereoselective pharmacokinetics in rats after an ig dose of the racemate.

关 键 词：dl-延胡索乙素 手性拆分 药代动力学 立体选择性 

分 类 号：R917.101[医药卫生—药物分析学]