栀灯注射液中栀子苷、灯盏花素的大鼠药代动力学初步研究

目的建立大鼠血浆样品中栀子苷和灯盏花素的高效液相色谱检测方法,并研究栀灯注射液在大鼠体内的药代动力学特征,为其剂量设置提供依据。方法大鼠尾静脉注射栀灯注射液高、中、低3个剂量后检测不同时间血浆中栀子苷和灯盏花素的浓度,并估算药代动力学参数。结果所建立的测定方法对灯盏花素的线性范围为0.2~40μg/mL,对栀子苷的线性范围为0.5~200μg/mL,回收率大于85%,日内及日间RSD均小于10%。静注给予栀灯注射液后,灯盏花素和栀子苷的平均消除半衰期分别为21.6和72.6 min,分布容积分别为0.23~1.24和0.37~1.05 L/kg。结论建立的大鼠血浆中灯盏花素和栀子苷HPLC测定方法适合于药代动力学研究。

Study on pharmacokinetics of genioside and breviscapine in rats in Zhideng injection

Purpose A RP-HPLC method was used to determine genioside and breviscapine in plasma and to study its pharmacokinetics in rat, respectively.Methods Rat plasma samples were collected after a single dose of Zhideng injection and pharmacokinetic parameters of genioside and breviscapine were estimated,respectively.Results A good linear relationship was obtained between 0.2-40.0 μg/mL for breviscapine, and 0.5-200.0 μg/mL for genioside.The recoveries from plasma were larger than 85%,and RSDs of inter-day asaay and intra-day assay were below 10%. The pharmacokinetic results showed that genioside and breviscapine were rapidly eliminated from plasma after iv administration of three doses of Zhideng injection.The mean half-life was 72.6 min and 21.6 min,respectively.Conclusion The established HPLC method was suitable for the pharmacokinetic study of genioside and breviscapine.