论文部分内容阅读
目的:探讨葛根素在正常和β-淀粉样蛋白所致痴呆模型大鼠(AD模型大鼠)体内的动力学过程。方法:AD模型组大鼠基底核定位注射A,β7天后灌胃500mg/kg葛根素注射液,正常组灌胃等剂量葛根素注射液。采用反相高效液相色谱法测定给药后不同时间点血浆样品中葛根素的药物浓度,3P87软件拟合药动学参数。结果:葛根素口服给药在正常和AD大鼠体内的药动学过程均为开放性一室模型。AD大鼠的半衰期(t1/2,m in)、药时曲线下面积(AUC,μg.m in-1.mL-1)、平均驻留时间(MRT,m in)、表观分布容积(Vd/F,L)分别为19.2、301.5、42.8、45.8;相对应的正常大鼠则为40.8、453.0、56.9、65.1。结论:葛根素在AD大鼠体内消除更快,半衰期与平均驻留时间缩短;从血浆中向其他组织的分布速率减慢。提示葛根素在AD病理状态下代谢、排泄速度更快。同时,葛根素在AD病理状态下更多地积蓄在血浆中。
Objective: To investigate the kinetics of puerarin in normal and β-amyloid induced dementia model rats (AD model rats). Methods: Rats in AD model were injected intraperitoneally with puerarin (500 mg / kg) 7 days after intraperitoneal injection of A and β, and the rats in normal group were given puerarin at the same dosage. The drug concentrations of puerarin in plasma samples at different time points after administration were determined by RP-HPLC and the pharmacokinetic parameters were fitted by 3P87 software. RESULTS: The pharmacokinetics of puerarin orally administered in both normal and AD rats were open-studio. The half-life (t1 / 2, m in), ADSI (AUC, μg.m in -1.mL-1), mean residence time (MRT, m in) and apparent volume of distribution Vd / F, L) were 19.2,301.5,42.8,45.8 respectively; corresponding normal rats were 40.8,453.0,56.9,65.1. CONCLUSION: Puerarin is faster in elimination, shorter in half-life and average residence time in AD rats, and slower in distribution from plasma to other tissues. Tip puerarin in AD pathological metabolism, excretion faster. At the same time, puerarin accumulates more in plasma in the pathology of AD.