中国中药杂志

2011, v.36(24) 3515-3518

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冬凌草甲素在小鼠体内的药代动力学研究
Study on pharmacokinetics of oridonin in mice

郑海娜;李吉学;姚会枝;
ZHENG Haina1,LI Jixue1,2,YAO Huizhi1 (1.Pharmacological College of Henan University,Kaifeng 475004,China; 2.Pharmacological Institute of Henan University,Kaifeng 475004,China)

摘要(Abstract):

目的:建立小鼠血浆中冬凌草甲素的高效液相测定方法,探讨冬凌草甲素在小鼠体内的药代动力学过程。方法:小鼠按10 mg.kg-1尾静脉注射冬凌草甲素后,不同时间点摘除眼球取血,乙酸乙酯萃取血浆,HPLC测定血浆中冬凌草甲素的浓度,并用3P97软件拟合,计算药动学参数。结果:冬凌草甲素在0.202~20.0 mg.L-1线性关系良好,r=0.998 7,测得低、中、高浓度方法回收率均大于93%,低、中、高浓度日内、日间精密度RSD均小于9%。冬凌草甲素小鼠尾静脉注射给药后,在体内呈二室模型分布,其药代动力学方程为C=16.192 5e-0.5546t+5.475 7e-0.0163t,主要药动学参数为t1/2α1.249 9 min,t1/2β42.638 4 min,K21 0.152 3 min-1,K12 0.359 3 min-1,K10 0.059 2 min-1,AUC 366.035 0μg.min-1.mL-1,CL 0.027 3 L.min-1.kg-1,VC 0.461 5 L.kg-1。结论:建立的RP-HPLC测定方法适用于体内冬凌草甲素的含量测定及药代动力学研究,冬凌草甲素在小鼠体内吸收快、分布也快,药物起效迅速,在体内以消除为主。
Objective: To develop a HPLC method for the determination of plasma concentration of oridonin(ORI) and study the pharmacokinetics of ORI in mice.Method: Blood was sampled from mice which were injected ORI by 10 mg·kg-1 at different time intervals,and the concentration of ORI was determined by HPLC.The pharmacokinetic parameters were accessed by 3P97.Result: The calibration curve was linear(r=0.998 7) within the range of 0.202-20.0 mg·L-1 for ORI in plasma.The average recoveries were more than 93%.The within-day and between-day precisions were no more than 9%.After iv oridonin in mice,the plasma concentration-time course fitted well to two-compartment model.The pharmacokinetic equation was C=16.192 5e-0.554 6t+5.475 7e-0.016 3t.The pharmacokinetic parameters were below: t1/2α 1.249 9 min,t1/2β 42.638 4 min,K21 0.152 3 min-1,K12 0.359 3 min-1,K10 0.059 2 min-1,AUC 366.035 0 μg·min·mL-1,CL 0.027 3 L·min-1·kg-1,VC 0.461 5 L·kg-1..Conclusion: The method can be used to determine the concentration and to investigate the pharmacokinetics of ORI in mice.ORI was absorbed and distributed very fast in mice.The effect of ORI was rapid.The elimination was the main process.

关键词(KeyWords): 冬凌草甲素;药代动力学;高效液相色谱;二室模型
oridonin;pharmacokinetics;HPLC;two-compartment model

Abstract:

Keywords:

基金项目(Foundation): 河南省教育厅自然科学研究指导计划项目(2010B350001);; 河南大学博士启动金项目

作者(Authors): 郑海娜;李吉学;姚会枝;
ZHENG Haina1,LI Jixue1,2,YAO Huizhi1 (1.Pharmacological College of Henan University,Kaifeng 475004,China; 2.Pharmacological Institute of Henan University,Kaifeng 475004,China)

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