小檗碱对葛根素在大鼠体内药动学的影响

摘要

Objective To observe the effect of berberine on pharmacokinetics of puerarin in rats.Methods Plasma puerarin concen-tration was determined by HPLC after intragastrical administration of puerarin(100 mg·kg-1 )or puerarin combined with berberine (50,100,200mg·kg-1 )in rats.The data were processed by DAS ver1.0 software to calculate the pharmacokinetic parameters.Re-sults Chromatographic peaks for puerarin were separated well by the HPLC method.Regression analysis of the data of puerarin con-centration against its peak area showed a good straight line in the range of 0.10~10.00 mg·L-1 (r=0.999 5).The main pharmaco-kinetic parameters of puerarin before and after coadministration of berberine were as follows:Cmax were (0.54 ±0.05),(0.59 ±0.03), (0.67 ±0.02),(0.73 ±0.03)mg·L-1;AUC0~∞ were (4.90 ±2.91),(4.63 ±2.11),(3.42 ±2.44),(6.18 ±2.57)mg·L-1 ·h-1;CL were(26.92 ±16.24),(25.94 ±13.36),(44.58 ±30.36),(18.82 ±8.47)L·h-1 ·kg-1 .Conclusions High dose of berberine can significantly enhance puerarin absorption in rats.%目的：观察小檗碱对葛根素在大鼠体内药动学的影响。方法建立高效液相色谱（HPLC）法测定大鼠血浆中葛根素的浓度。大鼠灌胃给予葛根素（100 mg·kg-1）及葛根素和小檗碱混合物（100 mg·kg-1＋50 mg·kg-1、100 mg·kg-1＋100 mg ·kg-1、100 mg·kg-1＋200 mg·kg-1），用HPLC法测定大鼠给药后不同时间血浆葛根素的浓度，DAS ver1．0数据处理软件计算药动学参数。结果葛根素在0．10～10．00 mg·L-1范围内线性良好（r＝0．9995）。合用小檗碱前后葛根素的主要药动学参数Cmax分别为（0．54±0．05）、（0．59±0．03）、（0．67±0．02）、（0．73±0．03）mg·L-1；AUC0～∞分别为（4．90±2．91）、（4．63±2．11）、（3．42±2．44）、（6．18±2．57）mg·L-1·h-1；CL 分别为（26．92±16．24）、（25．94±13．36）、（44．58±30．36）、（18．82±8．47）L·h-1·kg-1。结论高剂量小檗碱可提高葛根素在大鼠体内的吸收。