葛根素及其磷脂复合物在Beagle犬体内的药动学比较

Comparison of pharmacokinetics between puerarin and its phospholipid complex in Beagle dogs in vivo

目的研究葛根素及其磷脂复合物中葛根素在B eag le犬体内药动学。方法采用HPLC法测定犬血中葛根素,以同组犬(3只,雄性)交叉口服葛根素及其磷脂复合物,药-时曲线数据经3P 97药动学计算程序处理。结果分别以葛根素及其磷脂复合物给B eag le犬口服(剂量为葛根素52.5 m g/kg),葛根素的药-时过程符合开放型双室一级动力学模型,葛根素口服的AUC、Cm ax、tm ax分别为(10.91±4.83)m g.h/L、(3.00±1.13)m g/L、(1.62±0.30)h,而葛根素磷脂复合物的AUC、Cm ax、tm ax分别为(13.67±2.72)m g.h/L、(1.91±0.51)m g/L、(2.38±1.27)h,统计结果表明AUC之间差异有显著性。结论形成磷脂复合物可提高葛根素在B eag le犬体内的吸收。

Objective To study the pharmacokinetics of puerarin and its phospholipid complex in Beagle dogs in vivo. Methods To determine the puerarin concentration in blood by HPLC, carry on the cross-experiments in the same group of dogs, and calculate the data using 3P97 pharmacokinetic program software. Results The concentration-time profiles of puerarin after ig puerarin and its phospholipid complex （equivalent to 52.5 mg/kg of puerarin） were shown to fit two-compartment open model with first-order absorption. Their AUC, Cmax, and tmax for puerarin were （10.91±4.83） mg · h/L, （3.00± 1.13） mg/L, and （1.62±0.30） h, while for puerarin in phospholipid complex were （13.67±2.72） mg·h/L, （1.91±0. 51） mg/L, and （2.38±1.27） h, respectively. Difference in AUC is significant. Conclusion Phospholipid complex formation can effectively enhance puerarin absorption in Beagle dogs in vivo.