三七中3种皂苷类成分体内整合药动学研究  

INTEGRATED PHARMACOKINETICS OF THREE SAPONINS OF PANAX NOTOGINSENG IN VIVO

作　　者：赖玲[1] 刘华钢[1] 秦艳娥[1] 陆仕华[1] 文丽[2] 陈明 刘冠萍 

机构地区：[1]广西医科大学,南宁530021 [2]广西中医学院,南宁530001 [3]广西梧州制药(集团)股份有限公司,梧州543000

出　　处：《广西医科大学学报》2012年第2期193-196,共4页Journal of Guangxi Medical University

基　　金：广西企业科技特派员专项项目(No.09321049);广西自然科学基金资助项目(No.2010GXNSFB013068)

摘　　要：目的:考察三七中3种皂苷成分在大鼠体内各自的和整合的药动学特性,并分别计算绝对生物利用度。方法:SD大鼠分别灌胃及静脉注射剂量为600mg.kg-1及50mg.kg-1的三七总皂苷,采用HPLC法测定其中3种皂苷类成分三七皂苷R1、人参皂苷Rb1和人参皂苷Rg1不同时间间隔的血药浓度,运用3P97药动学程序计算各成分的药动学参数,利用各成分曲线下面积(AUC0→∞)百分率作为自定义权重系数,计算三七中3种皂苷在大鼠体内综合血药浓度,并建立整合药动学研究模型,进一步估算整合药动学参数。根据药时曲线的AUC面积计算绝对生物利用度。结果:给药后3种皂苷之间药动学参数差异很大,各成分在大鼠体内能快速分布并消除,两种给药途径的体内药动学过程均符合二室模型,3种成分及整合后绝对生物利用度分别是:1.76%、0.78%、2.44%和0.78%。结论:基于3种皂苷类成分的AUC0→∞自定义权重系数的整合药动学研究模型符合经典药动学模型特征,所获参数能够最大程度上表征中药的整体处置规律,该数据处理方法是对中药多组分整合药动学新方法的又一尝试。Objective：To investigate pharmacokinetics and bioavailability of three saponins of panax notoginseng after intragastric and intravenous administration of total panax notoginsenosides（PNS） in rats.Methods： Concentrations of panax notoginsenoside R1,ginsenoside Rb1 and Rg1 in rat plasma were determined by HPLC method after intragastric and intravenous administration of 600 mg/kg and 50 mg/kg dosage of PNS,respectively.Pharmacokinetic parameters of each compound were calculated using 3P97 software.A novel approach of self-defined weighting coefficient based on the area under the curve from zero to infinity（AUC0→∞） has been created to obtain the holistic pharmacokinetic profiles of PNS.The integrated pharmacokinetic parameters of PNS were then calculated from both typical compartment and non-compartmental model analysis.The absolute bioavailability was calculated based on the AUC0→∞values.Results： The pharmacokinetic parameters of three saponins were different from each other after intragastric and intravenous administration.They can be rapidly distributed and eliminated in rats.The pharmacokinetics of two routes of administration both are two compartments model.The absolute bioavailability of PNS was 1.76%,0.78%,2.44% and 0.78%,respectively.Conclusion： A novel integrated pharmacokinetic approach to describe the holistic pharmacokinetic properties of Chinese materia medica has been successfully developed and validated using three saponins of panax notoginseng as a model herbal medicine.This study would be a new try for guiding the holistic pharmacokinetic study in consistence with the intrinsic theory and characteristics of traditional Chinese medicine.

关 键 词：三七 皂苷 整合药动学 

分 类 号：R945[医药卫生—微生物与生化药学]