【摘要】 目的考察杠柳毒苷iv给药在大鼠体内的药动学过程。方法大鼠iv给予低、中、高剂量(0.37、0.74、1.48mg/kg)杠柳毒苷后于不同时间点采血,血浆样品经甲醇沉淀蛋白-C18固相萃取处理,HPLC-UV法测定不同时间点大鼠血浆中杠柳毒苷药物浓度。用DAS药动学数据软件计算药动学参数。结果低、中、高剂量组杠柳毒苷的分布相半衰期t1/2α分别为1.49、2.32、3.48min,消除相半衰期t1/2β分别为14.00、12.37、15.44min,无显著性差异。AUC0-60分别为8.581、19.782、50.615mg/L·min,与剂量呈线性相关。结论杠柳毒苷iv给药在大鼠体内分布及消除迅速,其体内过程符合二房室模型,在0.37～1.48mg/kg符合线性动力学过程。更多还原

【Abstract】 Objective To investigate the in vivo pharmacokinetic properties of periplocin from Periplocae Cortex in rats after iv injection.Methods Low,medium,and high dosage of periplocin were administered to rats respectively and blood was sampled at designed time points.Plasma samples were pretreated by protein precipitation with methanol,followed by solid-phase extraction with a C18 cartridge.Plasma concentrations of periplocin were determined by HPLC-UV method.Main pharmacokinetic parameters were calculated with DAS software.Results After single iv injection with doses of 0.37,0.74,and 1.48 mg/kg to rats,t1/2α of periplocin were 1.49,2.32,and 3.48 min,respectively;t1/2β were 14.00,12.37,and 15.44 min,respectively,without significant differences.AUC0-60 were 8.581,19.782,and 50.615 mg/L·min,respectively.The AUCs were found to be linearly correlated with dosages.Conclusion Periplocin shows the rapid distribution and elimination in rats after iv injection.Pharmacokinetics of periplocin fits best to a two-compartment model with first order kinetics.Amount of in vivo exposure is positively correlated with dosage over the dose range of 0.37—1.48 mg/kg.更多还原