熊胆降热丸中儿茶素在大鼠体内的药代动力学研究

Pharmacokinetic Study of Catechin in Xiongdan Jiangre Pills in Rats

目的研究熊胆降热丸中儿茶素在大鼠体内的药代动力学特性。方法以乙腈-水-三乙胺(6∶94∶0.3,磷酸调节pH=4.0±0.1)为流动相,血浆样品经甲醇-饱和硫酸锌(1∶1)除蛋白,采用高效液相色谱(HPLC)法测定儿茶素的浓度。利用DAS2.0软件计算儿茶素的主要药代动力学参数。结果儿茶素在0.12～9.6 mg/L范围内线性关系良好(r=0.999 2),平均绝对回收率为90.2%～97.1%,日内和日间RSD均低于15%。儿茶素大鼠体内的主要药代动力学参数Cmax为(1.670±0.754)mg/L,T1/2β为(7.779±4.568)h,AUC0-t为(6.192±2.828)mg/(L.h),AUC0-∞为(7.444±4.176)mg/(L.h)。结论该方法快速、准确、灵敏,可用于儿茶素的药代动力学研究,为儿茶药材和含儿茶中药复方制剂的体内研究和临床合理用药提供参考。

Objective To study the pharmacokinetic characteristics of catechin in Xiongdan Jiangre Pills in rats. Methods The mixture of acetonitrile-water-triethylamine （6：94：0.3,adjusting to pH（4.0 20. 1） with phosphoric acid） was used as the mobile phase. The plasma samples were pretreated by methanol and zinc sulfate aqueous solution（1 ： 1） for deproteinization,then analyzed by HPLC. The main pharmacokinetic parameters of catechin were calculated by the DAS 2.0 software. Results The linear range of catechin was 0.12-9.6 mg/L （r =0. 999 2）. Both the within-day and betweenday RSD were less than 15%. The average absolute recovery rate was 90. 2% -97. 1%. The main pharmacokinetic parameters were as follows： Cmax（1. 670 20. 754）mg/L, T1/2β（7. 779 24. 568）h, AUC0-t （6.192-＋2.828）mg/（L·h） and AUC0-∞（7.444±4.176）mg/（L· h）. Conclusion This method is rapid,accurate and sensitive,and can be used for the pharmacokinetic study of cateehin,which provides the pharmacokinetic evidence for the in vivo study and clinical rational medication of catechin medicinal materials and the compound Chinese medicine preparations containing catechin.