小檗碱对葛根素在大鼠体内药动学的影响

Effect of berberine on pharmacokinetics of puerarin 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=0.999 5）。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。

Objective To observe the effect of berberine on pharmacokinetics of puerarin in rats. Methods Plasma puerarin concentration 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. Results Chromatographic peaks for puerarin were separated well by the HPLC method. Regression analysis of the data of puerarin concentration 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 pharmacokinetic parameters of puerarin before and after coadministration of berberine were as follows：Cmaxwere（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.