LC/MS测定大鼠灌胃黄连提取物后血浆中小檗碱、巴马汀及其药物动力学研究  

LC /MS Determination of Berberine and Palmatin in Rats Plasma after Oral Administration of Extracts Rhizoma Coptidis and its Pharmacokinetics Study

作　　者：鲍天冬[1] 李玉洁[1] 杨庆[1] 翁小刚[1] 张英丰[1] 董宇[1] 王怡薇[1] 朱晓新[1] 

机构地区：[1]中国中医科学院中药研究所,北京100700

出　　处：《中国实验方剂学杂志》2010年第13期186-189,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家科学自然基金重点项目(30930114);国家自然科学基金项目(90709017);国家"十一五"科技支撑计划课题(2006BAI08B04-4)

摘　　要：目的:建立LC/MS测定大鼠血浆中小檗碱、巴马汀含量的方法,并探讨其在大鼠体内的药动学过程。方法:大鼠ig黄连提取物后不同时间点采血,LC-MS法测定血药浓度,并用Win Nonlin 5.1软件求算其药动学参数。结果:小檗碱、巴马汀质量浓度分别在5～1 000 ng·mL-1(r=0.998 9),2.5～500 ng·mL-1(r=0.999 4)线性关系良好。平均回收率大于85%,日内、日间RSD均小于15%。大鼠ig黄连提取物1.2,2.4,4.8 g·kg-1后,用非房室模型计算药动学参数,小檗碱的AUC平均值为707.91,1 220.32,2 424.62 h.ng-1·mL-1;T1/2平均值为1.89,2.29,4.79 h;Cmax平均值为:315.78,501.58,584.57 ng.mL-1;Tmax均为1 h;巴马汀的AUC平均值为:130.29,348.61,872.76 h.ng·mL-1;T1/2平均值为1.71,2.64,5.89 h;Tmax均为1 h;小檗碱和巴马汀的AUC与给药剂量之间呈现良好的线性关系。结论:该法专属性强,灵敏度高,可用于小檗碱、巴马汀的体内定量分析,小檗碱与巴马汀体内过程均符合一级速率过程。Objective：To develop an LC-MS method to determine berberine and palmatin in rats plasma simultaneously.The method was employed to investigate pharmacokinetics of berberine and palmatin.Method： Blood samples were collected at different time after oral administration of extracts Rhizoma Coptidis,The plasma concentration of berberine and palmatin was determined by LC-MS.Pharmacokinetic parameters were calculated by WinNonlin 5.1 software.Result：The linear range of berberine and palmatin was 5～1 000 ng·mL（r=9 989）,2.5～500 ng·mL^-1（r=9 994） respectively.The average recovery of berberine and palmatin was exceeded 85%（n=5）,the precision of inner-day and inter-day was less than 15%.The pharmacokinetics parameters calculated by noncompartment model,such as AUC,T1/2,Cmax of berberine were： 707.91 h·ng·mL-1,1 220.32 h·ng-1·mL^-1,2 424.62 h.ng-1·mL^-1;1.89 h,2.29 h,4.79 h;315.78 ng·mL^-1,501.58 ng^-1·mL^-1,584.57 ng·mL^-1;Tmax was all 1 h.The pharmacokinetics parameters AUC,T1/2.,Cmax of palmatin were： 130.29 h·ng^-1·mL^-1、348.61 h·ng^-1·mL^-1,872.76 h·ng^-1·mL^-1;1.71 h,2.64 h,5.89 h;Tmax was all 1 h.The relationship between dose and AUC showed good linearity.Conclusion： The method described in this report has high sensitivity and selectivity,and was suitable for pharmacokinetic studies of berberine and palmatin.The kinetic process of berberine in rats in vivo was fitted to a one-compartment model at low dosage,while it was fitted to two-compartment model at middle and high dosages;the kinetic process of palmatine was all fitted to a one-compartment model.

关 键 词：LC—MS 小檗碱 巴马汀 药物动力学 

分 类 号：R285.5[医药卫生—中药学]