葛根黄酮及其葛根素在正常和脑缺血再灌大鼠体内药动学比较

Studies on pharmacokinetics of pueraria flavonoid in normal and cerebral ischemia-reperfusion rats

目的 测定葛根黄酮及其中主要成分葛根素在正常和脑缺血再灌注大鼠体内的药动学的变化并作比较。方法 用荧光分光光度法 ,反相高效液相法分别测定给药后不同时间点葛根黄酮及其葛根素在正常和脑缺血再灌注大鼠体内的血药浓度。 3P87软件拟合药动学参数。结果 葛根黄酮及葛根素动力学均呈一室开放模型。正常和脑缺血再灌注状态下 ,葛根黄酮的t1/2 分别为 (34 3± 11 8)和 (43 7± 2 4 1)min ;葛根素的t1/2 分别为 (11 6± 1 2 )和 (15 8± 2 1)min。结论 缺血再灌注大鼠体内葛根素血药浓度高于正常大鼠 ,t1/2 明显延长 ,表明病理状态下 ,机体内药物代谢速率降低。葛根素及 3种未定性成分A ,B ,C在大鼠体内血药浓度消长变化基本一致 ,提示葛根素可以作为代表反映葛根黄酮中结构相似的多种成分在体内代谢过程。

OBJECTIVE To study the pharmacokinetics of puerarin and three unknown components in pueraria flavonoid (PF) in normal and cerebral ischemia-reperfusion rats. METHODS The blood samples at different times after administration were collected. The plasma concentrations of PF were determined by fluorescence spectrophotometer and those of puerarin and three unknown components were determined by RP-HPLC. The pharmacokinetic parameters were accessed by 3P87. RESULTS PF and puerarin were disposed as one-compartment model in normal and cerebral ischemia-reperfusion rats. In normal and cerebral ischemia-reperfusion rats, t 1/2 of PF and puerarin were (34.3±11.8) and (43.7±24.1)min;(11.6±1.2) and (15.8±2.1)min respectively. CONCLUSION There were many differences in pharmacokinetic parameters of PF and puerarin between normal and cerebral ischemia-reperfusion rats. The concentrations of PF and puerarin in ischemia-repefusion rats were higher and t 1/2 were longer than in normal rats. The differences of pharmacokinetics among puerarin, the unknown A, B and C were not significant which suggested that pharmacokinetics of puerarin in rats could be representative of the components with similar structure.