刺五加注射液中3个主要活性成分与相应单体在大鼠体内的药动学比较

研究刺五加注射液中3个活性成分，紫丁香苷、刺五加苷E及异嗪皮啶在大鼠体内的药动学行为，并与相应单体分别经静脉注射给药后大鼠体内药动学行为比较。将24只雄性大鼠随机分为4组，分别经静脉注射给予紫丁香苷、刺五加苷E、异嗪皮啶及相当剂量的刺五加注射液。采用液相色谱-串联四级杆质谱（liquid chromatography tandem mass spectrometry，LC-MS/MS）法测定不同时间点血浆中紫丁香苷、刺五加苷E及异嗪皮啶的浓度并采用DAS 2.0 数据处理软件及SPSS 17.0 统计软件分别进行药动学参数计算及比较。静脉给药后，3种单体成分与刺五加注射液主要药动学参数如血药浓度-时间曲线下面积（AUC）、血浆清除率（CL）、消除半衰期（t_1/2）等存在显著性差异（P<0.05）。刺五加注射液中紫丁香苷AUC较单体给药组明显增大，CL较单体给药组明显减小；刺五加苷E的AUC较单体给药组明显减小，CL较单体给药组明显增大；注射液中异嗪皮啶较单体给药组t_1/2延长。可见与单体给药相比，刺五加注射液中紫丁香苷、刺五加苷E及异嗪皮啶大鼠体内的代谢动力学过程存在差异。刺五加注射液中的其他共存成分可能对单个有效成分的主要药动学参数产生影响。

Comparative pharmacokinetics of syringin, eleutheroside E and isofraxidin in rat plasma after intravenous administration of each monomer and Ciwujia injection

To compare the pharmacokinetics of syringin, eleutheroside E and isofraxidin after intravenous administration of each monomer and Ciwujia injection. Twenty-four Sprague-Dawley rats were randomly divided into four groups and intravenously administrated with syringin, eleutheroside E, isofraxidin, and Ciwujia injection, respectively. The concentrations of the three components in rat plasma were determined by LC-MS/MS. DAS 2.0 software was applied to calculate the pharmacokinetic parameters while the SPSS 17.0 software was used for statistical analysis. Significant difference(P<0.05)was found between each monomer and the injection on the main pharmacokinetic parameters such as AUC, CL and t_1/2. Compared with the injection, the group treated with the syringin has obvious decrease in AUC, and increase in CL while the group treated with eleutheroside E has obvious increase in AUC, and decrease in CL. The t_1/2 of isofraxidin was prolonged in Ciwujia injection. Pharmacokinetic characters of the ingredients in the injection varied greatly from the monomer. Other constituents in the injection may have an impact on the pharmacokinetic profiles of these three components.