黄芪注射液对灯盏花素在糖尿病大鼠体内药动学的影响

Effect of Huangqi Injection on pharmacokinetics of breviscapine in diabetic rats

目的研究黄芪注射液对灯盏花素在糖尿病大鼠体内的药动学影响。方法将10只经链脲佐菌素诱导的糖尿病大鼠随机分为2组,A组静脉注射给予灯盏花素水溶液(16 mg/kg);B组在给予黄芪注射液(8 mL/kg)5 min后,静脉注射给予灯盏花素(16 mg/kg)。两组于给药后2、5、10、20、40、60、90、120、1802、40 min采集血样,采用HPLC测定灯盏花素的血药浓度,绘制药时曲线,用DAS 2.0计算药动参数,并对主要药动学参数进行统计学分析。结果灯盏花素单用或与黄芪注射液合用后,其在糖尿病大鼠体内的药动学过程均符合二室模型,且合用后灯盏花素的Tmax、Cmaxt、1/2α和t1/2β较单用时均无显著性差异(P>0.05),而Cl/F较单用灯盏花素时显著性减小(P<0.01),但AUC较单用灯盏花素时显著性增大(P<0.01)。结论黄芪注射液可降低灯盏花素在糖尿病大鼠体内的消除,从而提高了灯盏花素的生物利用度,提示糖尿病患者在两药合用时应适度降低灯盏花素的用药剂量。

AIM To study the effect of Huangqi Injection on pharmacokinetics of breviscapine in diabetic rats.METHODS Ten diabetic rats induced by Streptozotocin were randomly divided into two groups.A group was intravenously administered with breviscapine at a single dose of 16 mg/kg,and B group was administered intravenously with breviscapine（16 mg/kg）after 5 min rats being intravenously administered with Hangqi Injection.The rats blood samples were collected at 2,5,10,20,40,60,90,120,180,and 240 min,and the plasma concentrations of breviscapine were determined by HPLC.According to the curve of concentration-time,the software of DAS 2.0 was used to estimate the pharmacokinetic parameters.RESULTS There was no significant difference between the two groups in the pharmacokinetic parameters of breviscapine,such as Tmax,Cmax,t1/2α and t1/2β（P〉0.05）,but Cl/F decreased and AUC increased when co-administering with Huangqi Injection（P〈0.01）.CONCLUSION Huangqi Injection could decrease the Cl/F of breviscapine,and improve the bioavailability of breviscapine in diabetic rats,which suggests that the dose of breviscapine should reduce when co-administering with Huangqi Injection in diabetic patients.