灯盏花素在正常大鼠和糖尿病大鼠体内的药动学差异

Pharmacokinetics of breviscapine in normal and diabetic rats

目的研究灯盏花素在正常大鼠和糖尿病大鼠体内的药动学差异。方法将5只正常Wistar雄性大鼠作为正常对照组,再将经链脲佐菌素造模的5只糖尿病大鼠作为实验组,每组大鼠分别按16mg/kg的剂量静脉给予灯盏花素,于不同时间点采集血样,处理后,经高效液相色谱测定血药浓度,绘制灯盏花素平均药时曲线图,用DAS 2.0拟合药动参数,对比实验组和正常对照组的药动学差异。结果灯盏花素在糖尿病大鼠体内的药动学参数药物达峰浓度、分布半衰期、消除半衰期和药时曲线下面积增大,清除率减小,差异有统计学意义(P<0.05)。结论灯盏花素在糖尿病大鼠和正常大鼠体内的药动学有显著性的差异,可能与糖尿病大鼠肝、肾功能受损有关,临床用药时应适当减小糖尿病患者灯盏花素的用药剂量。

Objective To study the pharmacokinetic differences of breviscapine in normal and diabetic rats. Methods Five male Wistar rats were divided as control group, and five diabetic rats induced by streptozotocin were divided as examined group. Both groups were intravenously administered with breviscapine at a single dose of 16 mg/kg. The blood samples were collected at different times, and the concentration of breviscapine in plasma were determined by HPLC. According to the curve of concentration-time, the software of DAS 2.0 was used to process the pharmacokinetic parameters. Results There were great differences between control and exam- ined groups. Peak concentration, distributing half life, clean up half life, and area under curve significant increased while clearance significant decreased （P 〈0.05）. Conclusion Breviscapine has significantly different pharmacol：inetics in diabetic rats and normal ones owing to the damage of the liver and kidney of the diabetic rats, which suggests the dose of breviscapine should be reduced when administered in diabetic patients.