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期 刊 ：中国中药杂志 2008年 33卷 11期 页码：1294.

关键词：乙腈沉淀法；甘草次酸；血药浓度；二室模型；

Keywords:precipitate by acetonitrile, glycyrrhetic acid, plasma concentration, two compartments modal,

摘 要 ：目的：建立大鼠血浆中甘草次酸浓度的高效液相测定方法，探讨甘草次酸在大鼠体内的药动学过程。方法：大鼠按1.0 mg·kg^-1尾静脉注射甘草次酸后0.08，0.17，0.25，0.33，0.5，0.75，1，2，3，4，6 h眼底采血，乙腈沉淀血浆，HPLC测定血浆中甘草次酸浓度，以DAS软件拟合药动学参数。结果：甘草次酸血药浓度在50～2 000 ng·mL^-1线性良好，r=0.999 7，测得低中高浓度回收率分别为(105.2 ±2.23)%，(102.5±2.95)%，(98.4±2.32)%，日内、日间低中高浓度RSD均小于4%。甘草次酸在大鼠体内药-时曲线符合二室开放模型，主要药动学参数为：t_1/2α=(0.153±0.023) h，t_1/2β=(2.365±0.866) h，C_max =(2.074±0.100) mg·L^-1，CL=(0.715±0.082) L·h^-1·kg^-1，V_d =(2.427±0.872) L·kg^-1，AUC_{0～6 h} =(1.302±0.151) mg·h^-1·L^-1。结论：建立的RP-HPLC适用于体内甘草次酸的含量测定及药代动力学研究，甘草次酸在体内的分布迅速、广泛。

Abstract:Objective: To develop a HPLC for the determination of plasma concentration of glycyrrhetic acid (GA) and study the pharmacokinetics of GA in rats. Method: To sample blood from rat which were injected GA by 1.0 mg·kg^-1 at 0.08，0.17，0.25，0.33，0.5，0.75，1，2，3，4，6 h and use HPLC to determine the concentration of GA in it, the pharmaeokinetie parameters were accessed by DAS 1.0. Result: The calibration curve was linear (r=0.999 7) within the range of 50-2 000 ng·mL^-1 for GA in plasma. The average recovery was (105.2±2.23)%, (102.5±2.95)%, (98.4±2.32)%. The within-day and between-day derivation (RSD) were less than 4%. GA was fitted to a two compartment open pharmaeokinetie model in rats. The mainly pharmaeokinetie parameters were: t_1/2α=(0.153±0.023) h, t_1/2β=(2.365±0.866) h, C_max=(2.074±0.100) mg·L^-1, CL=(0.715±0.082) L·h^-1·kg^-1, V_d=(2.427±0.872) L·kg^-1, AUC_{0-6 h}=(1.302±0.151) mg·h^-1·L^-1. Conclusion: The method can be used to determine the concentration and to investigate the pharmacokinetics of GA in rat. GA was disposed extensively and rapidly in rats.

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