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目的对于静脉注射葛根提取物后正常和心肌缺血大鼠体内葛根素药动学特征进行研究。方法大鼠尾静脉注射葛根提取物20 mg/kg后0.083 h、0.167 h、0.333 h、0.50 h、0.75 h、1.0 h、1.5 h、2 h、4 h、6 h、8 h对大鼠进行眼眶静脉丛采血,应用高效液相法测定血浆中葛根素的含量。结果正常组和病理组大鼠体内葛根素药动学过程均符合二室模型,正常组的药物分布相与消除相半衰期分别为7.2707 min与77.731 min,平均滞留时间MRT(0-∞)为141.61 min,AUC(0-∞)为2063.064 mg/L*h。病理组的药物分布相与消除相半衰期分别为11.372 min与101.342 min,平均滞留时间MRT(0-∞)为152.9 min,AUC(0-∞)为3219.091 mg/L*h。结论葛根提取物静脉注射后,药物在体内滞留时间短,分布和消除均较快。葛根素在正常组和病理组的大鼠体内的药动学均符合二房室模型,且尾静脉注射后病理组大鼠血药浓度普遍高与正常组,消除速度与正常组相比较慢。
Objective To study the pharmacokinetics of puerarin in normal and myocardial ischemic rats after intravenous injection of Pueraria lobata extract. Methods Rats were injected with Pueraria extract 20 mg / kg into the caudal vein at the time points of 0.083 h, 0.167 h, 0.333 h, 0.50 h, 0.75 h, 1.0 h, 1.5 h, 2 h, 4 h, 6 h, 8 h Orbital venous plexus blood collection, determination of plasma puerarin content using high performance liquid chromatography. Results The pharmacokinetics of puerarin in both normal and pathological groups were in accordance with the two-compartment model. The drug distribution phase and elimination half-life in normal group were 7.2707 min and 77.731 min, respectively, and the average residence time MRT (0-∞) was 141.61 min and AUC (0-∞) was 2063.064 mg / L * h. Pathological group drug distribution phase and elimination phase half-life of 11.372 min and 101.342 min, the average residence time MRT (0-∞) was 152.9 min, AUC (0-∞) was 3219.091 mg / L * h. Conclusion Pueraria extract intravenous injection, the drug in the body retention time is short, the distribution and elimination are fast. The pharmacokinetics of puerarin in both normal and pathological groups were in accordance with the two-compartment model. The plasma concentrations of puerarin in rats in the pathological group were generally higher and normal than those in the normal group, and the elimination rate was slower than that in the normal group.