梓葛冻干粉针中葛根素在大鼠肝肾的分布

目的:考察梓葛冻干粉针中葛根素在大鼠肝、肾的分布过程,探讨梓葛冻干粉针的安全性。方法:设梓葛冻干粉针药物组和葛根素冻干粉针对照组,按葛根素剂量26.7 mg.kg-1,经大鼠尾静脉给药。采用高效液相色谱法测定给药后5,10,20,30,45,60,120 min,大鼠肝、肾组织中葛根素的浓度。结果:药物组中葛根素在肾脏的峰浓度Cmax为58.12μg.g-1,药-时曲线下面积AUC0-2 h为26.24μg.h.g-1,平均滞留时间MRT0-2 h为0.39 h;对照组中葛根素在肾脏的Cmax71.28μg.g-1,AUC0-2 h35.24μg.h.g-1,MRT0-2 h0.42 h。与对照组相比,药物组大鼠肾脏中的葛根素Cmax和AUC0-2 h明显降低(P<0.05),达峰时间tmax和MRT0-2 h无显著性差异。2组中葛根素在肝脏的tmax,Cmax,AUC0-2 h和MRT0-2 h均无显著性差异。结论:与葛根素冻干粉针相比,梓葛冻干粉针中葛根素在肾脏的分布明显降低,消除无明显变化;在肝脏的分布与消除均无明显变化。说明梓醇可降低葛根素在肾脏中的分布,梓葛冻干粉针比葛根素粉针对于肾脏安全性更高。

Distribution of puerarin contained in Zige freeze-dried powder injection in rat liver and kidney

Objective: To investigate the distribution process of puerarin contained in Zige freeze-dried powder injection in rat liver and kidney and the safety of Zige freeze-dried powder injection.Method: Rats were divided into the Zige freeze-dried powder injection group and the puerarin freeze-dried powder injection control group randomly.The liver and kidney samples were collected at 5,10,20,30,45,60 and 120 min after intravenous administration of puerarin(26.7 μg·g-1) through caudal vein and detected by HPLC.Result: The concentration of puerarin in kidney reached the max value of 58.12 μg·g-1 for the Zige freeze-dried powder injection group and 71.28 μg·g-1 for the Puerarin freeze-dried powder injection group.The value of AUC0-2 h was 26.24 μg·h·g-1 for the Zige freeze-dried powder injection group and 35.24 μg·h·g-1 for the puerarin freeze-dried powder injection group,MRT0-2 h was 0.39 h for the Zige freeze-dried powder injection group and 0.42 h for the puerarin freeze-dried powder injection control group.Compared with the control group,the Zige freeze-dried powder injection group showed a significant decrease in Cmax and AUC0-2 h(P<0.05),with no notable difference in peak time tmax and MRT0-2 h.The two groups showed no obvious difference in tmax,Cmax,AUC0-2 h and MRT0-2 h of puerarin in rat kidney.Conclusion: Compared with Zige freeze-dried powder injection,Zige freeze-dried powder injection can reduce the distribution of puerarin in rat kidney,with no obvious change in the elimination of puerarin in rat kidney.It also showed no significant change in distribution and elimination in liver.This indicates that Zige freeze-dried powder injection is safer to kidney than puerarin freeze-dried powder injection.