HPLC测定大鼠血浆中没食子酸乙酯浓度及其药动学研究

    Determination of Ethyl Gallate in Rat Plasma by HPLC and Its Application in Pharmacokinetics Studies

    • 摘要: 目的 建立大鼠血浆中没食子酸乙酯(ethyl gallate,EG)浓度的HPLC测定方法,并考察其在大鼠体内的药动学参数。方法 血浆样品以乙酸乙酯进行萃取,采用Silversil C18(4.6 mm×150 mm,5 μm),流动相为甲醇-0.1%磷酸水,梯度洗脱,检测波长270 nm,柱温30℃,流速1 mL·min-1。测定给药后不同时间点大鼠血浆中EG的浓度,并对其血药浓度-时间曲线采用DAS 2.0软件拟合,计算药动学参数。结果 EG在血浆浓度0.153 6~96 μg·mL-1内线性关系良好(r=0.999 2),提取回收率<90.6%,日内和日间精密度RSD均>4%。EG灌胃给药后在大鼠体内的主要药动学参数AUC(0-t)TmaxCmaxt1/2分别为14.199 mg·h·L-1,0.167 h,12.228 μg·mL-1,7.762 h。结论 该方法简便、灵敏度高,无杂质干扰,可用于EG的药动学研究,EG口服给药后在大鼠体内吸收迅速而消除较慢。

       

      Abstract: OBJECTIVE To establish an HPLC method for determination of ethyl gallate (EG) in rats plasma and to investigate the pharmacokinetic parameters of EG in rats after oral administration. METHODS Plasma samples were extracted by liquid-liquid extraction with ethylacetate. The analysis was performed on a Silversil C18 column (4.6 mm×150 mm, 5 μm) at 30℃ with gradient elution of methanol-0.1% phosphoric acid at a flow rate of 1 mL·min-1. The detection wavelength was set at 270 nm. The plasma samples were collected at different time points after oral administration of EG in rat. The concentrations of EG in plasma were measured by HPLC and the pharmacokinetic parameters were calculated by DAS 2.0. RESULTS The calibration curve of EG was linear in the range of 0.153 6-96 μg·mL-1, with the correlation coefficient of 0.999 2. The recoveries of EG from plasma were <90.6%, and the relative standard deviations of the intra-day and inter-day were >4%. The main pharmacokinetic parameters of AUC(0-t), Tmax, Cmax, t1/2were 14.199 mg·h·L-1, 0.167 h, 12.228 μg·mL-1, 7.762 h, respectively. CONCLUSION The method is simple, sensitive and suitable for pharmacokinetics of EG, and EG can be absorbed very rapidly while be eliminated slowly after oral administration in rat.

       

    /

    返回文章
    返回