葛根提取物在正常及心肌缺血大鼠体内药物代谢动力学研究

Pharmacokineics of puerarin crude extract in normal and myocardial ischemia rats

目的对葛根提取物在正常和心肌缺血2种不同情况下大鼠体内的药物代谢动力学过程进行研究。方法正常大鼠及心肌缺血大鼠灌胃给予葛根提取物后（相当于葛根素600 mg·kg-1）在不同时间点眼眶采血,色谱甲醇沉淀蛋白,反相高效液相法测定各时间点葛根素在大鼠体内的的血药浓度,利用药动学软件DAS2.1.1拟合药动学参数。结果正常大鼠和心肌缺血大鼠血液中葛根素浓度药动学均符合二室模型,比较2组主要药动学参数,葛根素在正常及血肌缺血大鼠体内的AUC0~∞、AUC0~t分别为（990.764±42.3254）、（1236.914±1125.3）mg·min·L-1,（739.503±99.232）、（1210.016±111.12）mg·min·L-1,Cmax分别为（8.987±2.890）、（24.75±2.666）mg·L-1。结论与正常组大鼠相比,葛根素在心肌缺血大鼠体内血药浓度高,吸收速度快。反映了葛根对症治疗心肌缺血证疾病的临床合理性,体现了方与证相对应的中医思想。

Objective To study the pharmacokinetics of puerarin crude extract in the normal and myocardial ischemia rats. Methods The normal and myocardial ischemia rats received puerarin crude extract （equivalent of 600 mg · kg - 1 puerarin） by oral administration respectively. We took blood samples at different times, the protein was precipitated by chromatographic methanol, and the plasma concentration of the puerarin was analyzed by HPLC. The data were pro- cessed by DAS2.1.1 software to calculate the pharmacokinetic parameters. Results The pharmacokinetics of puerarin best fit the two-compartment models in normal and myocardial ischemia rats. The two groups of main pharmacokinetic parameters were： AUC0-∞ （990.764±42.3254） mg · min· L-1, AUC0-t（1236.914±1125.3） mg · min · L- 1 and Cmax （8.987±2.890） mg·L^-1 in the normal group; AUC0-∞ （1236.914± 1125.3） mg·min·L-1, AUC0-t（1210.016± 111.12） mg ·min· L - 1 and Cmax （24.75 4± 2.666） mg · L - 1 in the myocardial ischemia group. Conclusion Compared with the normal group, puerarin in myocardial ischemia rats has higher blood drug concentration and the absorption is faster. Puerarin may be used for symptomatic treatment of myocardial ischemia.