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Journal of ZheJiang University(Medical Science)  2012, Vol. 41 Issue (1): 6-12    DOI: 10.3785/j.issn.1008-9292.2012.01.002
    
Pharmacokinetics interaction among three major active compounds of Shengmai formula in rats
GUO Wen-jing,SHAO Qing,ZHANG Yu-feng,FAN Xiao-hui
Institute of Pharmaceutical Informatics,Zhejiang University,Hangzhou 310058,China
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Abstract  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.


Key wordsGinsenoside/pharmacokinetics      Schisandra chinensis/pharmacokinetics      schisandrin; Shengmai powders; Drug synergism      Chromatography, high pressure liquid; Mass spectrometry     
Published: 25 January 2012
Cite this article:

. Pharmacokinetics interaction among three major active compounds of Shengmai formula in rats. Journal of ZheJiang University(Medical Science), 2012, 41(1): 6-12.

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https://www.zjujournals.com/med/10.3785/j.issn.1008-9292.2012.01.002     OR     https://www.zjujournals.com/med/Y2012/V41/I1/6


生脉方主要活性成分配伍对其药代动力学行为的影响

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。

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 
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