杠柳毒苷在大鼠体内的药动学研究
首发时间:2011-01-18
摘要:目的采用静脉给药考察杠柳毒苷在大鼠体内的动态变化规律,为临床用药提供依据。方法建立HPLC法测定血浆中的杠柳毒苷药物浓度,测定大鼠体内药物动力学参数。结果该试验采用的高效液相法具有较高的专属性,在血药浓度为0.025~10.0μg/mL 范围内线性良好,有良好的相关系数(r=0.9988)。测定血浆中药物浓度,用DAS2.0拟合药动学参数。三个剂量的分布相半衰期t1/2α和消除相半衰期t1/2β分别为1.49 和 14.00min, 2.32 和12.37min, 3.48 和 15.44min。三个剂量的AUC0-60 和Cmax 分别为8.5814和1.076, 19.7821和2.337, 50.6151和5.816 (μg/mL)。结论杠柳毒苷在大鼠体内迅速分布、快速消除。药时曲线下面积AUC及平均最大血药浓度Cmax等参数与剂量线性相关,符合线性动力学特征。表观分布容积(Vd)、K12和清除率(CL)随给药剂量的倍增呈对应倍数下降。
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Pharmacokinetics research on Periplocin in rats
Abstract:【Objective】the pharmacokinetic of periplocin was studied through administered i.v. via tail vein. to provide a basis for clinical medicine. 【Methods】HPLC method was established to determine the Periplocin in plasma and measure the pharmacokinetic parameters in rats. 【Results】The experiment with high-performance liquid method has higher specificity, with satisfactory linearity in the plasma concentration range of 0.025~10.0μg/mL and good correlation coefficient (r=0.9988). Pharmacokinetic parameters were calculated with DAS2.0 practical pharmaeokinetics program. The adsorption half-life time (t1/2α) and elimination half-life time (t1/2β) of three dose was 1.49 and 14.00min, 2.32 and 12.37min, 3.48 and 15.44min, respectively. The AUC0-60 (mg/L*min) and Cmax (μg/mL) of three dose was 8.5814 and 1.076, 19.7821 and 2.337, 50.6151 and 5.816, respectively. All of these indicated the rapid distribution, elimination and linear kinetics pharmacokinetic characteristics of periplocin in rats after intravenously dosed.
Keywords: Periplocin HPLC pharmacokinetics
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No.4405602563490129****
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