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目的:建立类叶升麻苷血药浓度的高效液相色谱测定方法,并探讨其在大鼠体内的药代动力学特点。方法:SD大鼠6只,灌胃类叶升麻苷150 mg·kg-1后,于不同时间点采血,采用反相高效液相色谱法测定其血药浓度变化,并用DAS2.0软件拟合并计算药动学参数。结果:类叶升麻苷血药浓度的回归方程为Y=3.509 8X-0.096 8,r=0.996 8,在0.125～2.5mg·L-1线性关系良好。方法回收率均大于85%,日间及日内精密度的RSD均小于15%,符合生物样品分析要求。大鼠灌胃给药150 mg·kg-1的类叶升麻苷后,血浆中的类叶升麻苷的药时曲线呈二室开放模型,主要药动学参数Tmax,Cmax,t1/2α,t1/2β,AUC0-t,AUC0-∞,CL/F,V/F,Ka分别为0.361 h,1.126 mg·L-1,0.759,4.842 h,3.134,3.766 mg·h·L-1,87.089 L·h-1·kg-1,207.704 L·kg-1,6.345 h-1。结论:建立了类叶升麻苷血药浓度方法,该方法专属性强,灵敏度高,可用于该药的体内定量分析。
OBJECTIVE: To establish a HPLC method for the determination of plasma concentration of acteoside and study its pharmacokinetics in rats. Methods: Six Sprague-Dawley rats were fed with 150 mg · kg-1 of acteoside and the blood samples were collected at different time points. The changes of plasma concentration were determined by RP-HPLC. The pharmacokinetic parameters were calculated. Results: The regression equation of plasma concentration of acteoside was Y = 3.509 8X-0.096 8, r = 0.996 8, and the linearity was 0.125-2.5 mg · L-1. The recovery rates of the methods were both higher than 85%. The RSDs of intra-day and intra-day precision were less than 15%, which met the requirements of biological sample analysis. After oral administration of 150 mg · kg-1 of acteoside, the pharmacokinetic parameters Tmax, Cmax, t1 / 2α in plasma of rats were two-compartment open model. , t1 / 2β, AUC0-t, AUC0-∞, CL / F, V / F and Ka were 0.361 h, 1.126 mg · L-1, 0.759 and 4.842 h, 3.134 and 3.766 mg · h · L -1, 87.089 L · h-1 · kg-1, 207.704 L · kg-1, and 3.455 h-1. Conclusion: The method of plasma concentration of acteoside was established. The method is characterized by strong specificity and high sensitivity, and can be used for in vivo quantitative analysis of the drug.