青天葵中鼠李柠檬素在大鼠体内的药代动力学研究

目的 研究青天葵中鼠李柠檬素在大鼠体内的药代动力学特征.方法以甲醇一乙腈-0.2％磷酸水溶液（30∶35∶35）为流动相,血浆样品经10％三氯乙酸沉淀蛋白后,采用高效液相色谱法测定鼠李柠檬素的血药浓度.采用DAS 2.1.1药代动力学软件计算鼠李柠檬素的主要药代动力学参数.结果 鼠李柠檬素质量浓度在0.05～10.00 μg/mL范围内与峰面积线性关系良好（r=0.9993）,回收率为98.1％ ～ 101.1％,日内和日间RSD均小于11％.鼠李柠檬素大鼠体内符合二室模型,主要药代动力学参数峰浓度（Cmax）为（875.37±65.53）μg/L,药物消除半衰期（t1/2β）为（8.993±2.568）h,0 ～24h药时曲线下面积（AUC0-24）为（4929.159±589.652）μg· h/L,0～∞药时曲线下面积（AUC0-x）为（5 945.567±612.985）μg·h/L.结论鼠李柠檬素的药代动力学研究结果为青天葵药材的质量评价奠定了良好基础.

Pharmacokinetics of Rhamnocitrin in Ford Nervilia Leaf in Rat

Objective To study the pharmacokinetics of rhamnocitrin in Ford nervilia leaf in rats.Methods The mixture of methanolacetonitrile-0.2％ phosphoric acid （30：35：35） was used as the mobile phase.After precipitating protein by 10％ trichloracetic acid,plasma samples were determined the rhamnocitrin concentration by high performance liquid chromatography（HPLC）.The main pharmacokinetics parameters were calculated by the DAS 2.1.1 pharmacokinetic software.Results The rhamnocitrin mass concentration in the range of 0.05-10.00 μg/mL had the good relation with the peak area（r=0.999 3）.The recovery rate was 98.1％-101.1％.Both within-day and between-day RSD were less than 11％.The plasma concentration-time curve of rhamnocitrin fitted to the two-compartment model.The main pharmacokinetic parameters were as follows：Cmax =（875.37 ＋ 65.53） μg/L,T1/2β =（8.993 ± 2.568）h,AUC（0-24） =（4 929.159 ± 589.652） μg · h/L,AUC（0-∞） =（5 945.567 ± 612.985） μg · h/L.Conclusion The pharmacokinetic study results of rhamnocitrin provided a good foundation for the quality evaluation of Ford nervilia leaf.