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目的 观察厚朴酚与和厚朴酚在Wistar大鼠体内的动力学过程。方法 用实验建立的RP -HPLC法测定大鼠灌胃给予上述两种成分后不同时间各组织和体液中药物的含量及其蛋白结合率 ,并计算其在血中的药代动力学。结果 建立的方法能够良好分离两种成分 ,浓度 -色谱响应间线性相关系数均 >0 .999,平均加样回收率 >90 % ;两种成分在大鼠体内代谢符合一级消除动力学二室开放模型 ,Cmax 分别为 0 .974和 0 .5 2 2mg·L-1,T1/ 2 β 为 3.136和 3.2 84h ,T1/ 2ka 为 0 .16 0和 0 .2 6 1h ;进入体内后 ,主要滞留于胃肠内 ,其他主要分布于肝、肺、肾组织中 ;血浆蛋白结合率分别为 6 8.5 4 %和 5 3.81% ;以粪排出为主 ,尿和胆汁排出量只有约 5 %。结论 厚朴酚与和厚朴酚吸收较差 ,进入循环后以肝代谢和肾排泄为主。
Objective To observe the kinetics of honokiol and honokiol in Wistar rats. Methods The RP-HPLC method was used to determine the content and protein binding rate of various drugs in various tissues and body fluids after intragastric administration of the above two components at different times, and the pharmacokinetics in blood was calculated. Results The established method was able to separate the two components well. The linear correlation coefficient between concentration-chromatographic response was more than 0.999, and the average recovery rate was more than 90%. The metabolism of the two components in rats was in line with the first-order elimination kinetics. In the open model, Cmax was 0.974 and 0.52 2 mg·L-1, T1/ 2 β was 3.136 and 3.2 84 h, and T1/ 2ka was 0. 16 0 and 0.22 1 h. Retention in the gastrointestinal tract, the other mainly distributed in the liver, lung, kidney tissue; plasma protein binding rate was 68.54% and 5 3.81%; mainly fecal discharge, urine and bile output was only about 5%. Conclusion The absorption of honokiol and honokiol is poor, and the metabolism and renal excretion are the main factors after entering the circulation.