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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 establish a method for the determination of berberine and palmatine in rat plasma by LC / MS and investigate its pharmacokinetics in rats. Methods: Blood samples were taken from rats at different time points after the extract of Coptis chinensis and the plasma concentration was determined by LC-MS. The pharmacokinetic parameters were calculated by Win Nonlin 5.1 software. RESULTS: The berberine and palmatine concentrations were good at 5-1000 ng · mL-1 (r = 0.998 9) and 2.5-500 ng · mL-1 (r = 0.999 4) respectively. The average recovery rate is greater than 85%, intraday, daytime RSD were less than 15%. Pharmacokinetic parameters were calculated using the non-compartmental model after the rats were given ig.1. 2, mL-1; average T1 / 2 was 1.89,2.29,4.79 h; mean Cmax was 315.78, 501.58, 584.57 ng.mL-1; Tmax was 1 h; mean AUC of palmatine was 130.29, 348.61,872.76 h.ng · mL-1; average T1 / 2 was 1.71,2.64,5.89 h; Tmax was 1 h; the AUC of berberine and palmatine showed a good linear relationship with the dose . Conclusion: The method is highly specific and sensitive, and can be used for the quantitative analysis of berberine and palmatine in vivo. The in vivo process of berberine and palmatine all accord with the first order rate process.