生脉方主要活性成分配伍对其药代动力学行为的影响  

Pharmacokinetics interaction among three major active compounds of Shengmai formula in rats

作　　者：郭文婧[1] 邵青[1] 张玉峰[1] 范骁辉[1] 

机构地区：[1]浙江大学药物信息学研究所,浙江杭州310058

出　　处：《浙江大学学报（医学版）》2012年第1期6-12,共7页Journal of Zhejiang University(Medical Sciences)

基　　金："重大新药创制"国家科技重大专项(No.2009ZX09502-005);国家自然科学基金项目(No.81173467)

摘　　要：目的:建立液质联用测定大鼠血清中人参皂苷Rg1、人参皂苷Rb1和五味子醇甲的方法,用于研究生脉方中这3种成分配伍前后药动学行为的差异。方法:采用人参皂苷Rg1、人参皂苷Rb1和五味子醇甲3种化合物分别给大鼠单独或同等剂量配伍(100 mg.kg-1)灌胃。血清样品液萃取,LC-MS分析检测。用WinNonLinu6.0,以非房室模型计算药动学参数。结果:配伍给药组与单体给药组相比,人参皂苷Rg1的达峰浓度由(0.476±0.238)μg.ml-1上升为(1.946±1.432)μg.ml-1,AUC0-∞由(0.523±0.238)μg.h.ml-1上升为(1.908±1.319)μg.h.ml-1,CL由(226311±96819)ml.h-1.kg-1下降为(90650±73684)ml.h-1.kg-1,Vd由(317110±154009)ml.kg-1下降为(130967±78306)ml.kg-1。人参皂苷Rb1和五味子醇甲的药动学参数无明显变化。结论:配伍给药后,人参皂苷Rg1的生物利用度有显著提高,而人参皂苷Rb1、五味子醇甲的药动行为无明显差异。Objective： To investigate the pharmacokinetic interaction among three major bioactive compounds of Shengmai formula. Methods： After oral administration of ginsenoside Rg1,ginsenoside Rb1 and schisandrin with the same dose（100 mg·kg-1） individually or in combination,rat serum samples were extracted,then these three compounds were determined by liquid chromatography-mass spectrometry（LC-MS）.The pharmacokinetic parameters of three compounds in single or combination form were calculated by WinNonLinu6.0 using non-compartment model. Results： Compared with single drug group,the peak concentration of ginsenoside Rg1 in combined group increased from（0.476±0.238）μg·ml-1 to（1.946±1.432）μg·ml-1,AUC0-∞ increased from（0.523±0.238）μg·h·ml-1 to（1.908±1.319）μg·h·ml-1,CL decreased from（226311±96819）ml·h-1·kg-1 to（90650±73684）ml·h-1·kg-1 and Vd decreased from（317110±154009）ml·kg-1 to（130967±78306）ml·kg-1.While the pharmacokinetic parameters of ginsenoside Rb1 and schisandrin showed no significant change. Conclusions： Combined oral administration of three compounds of Shengmai formula can improve the bioavailability of ginsenoside Rg1,however it does not change the pharmacokinetic behavior of ginsenoside Rb1 and schisandrin.

关 键 词：人参皂甙/药代动力学 五味子/药代动力学 五味子醇甲 生脉散 药物协同作用 色谱法 高压液相 质谱分析法 

分 类 号：R284[医药卫生—中药学]