【摘要】 目的　研究天麻素在大鼠体内的药动学 ,探讨其在大鼠体内的动力学特征。方法　采用胆管结扎术和颈静脉插管术 ,同时建立高效液相色谱法测定血浆中天麻素浓度的变化 ,应用 3P87药动学程序对血药浓度数据进行拟合。结果　天麻素在2 5～ 80 0 μg·mL- 1 浓度范围内样品峰面积与内标峰面积比呈良好线性关系 ,其相关系数r=0 .995。提取平均回收率 83 .6 % ,日内、日间RSD <1 5 %。大鼠静脉注射天麻素后体内药动学符合开放性双隔室模型 ,而灌胃给药符合开放性单隔室一级吸收模型 ,其绝对生物利用度为 86 .1 %。大鼠结扎胆管前后AUC0～ 1 80 分别为 (1 8± 9) ,(1 5± 1 3)mg·min·mL- 1 ,经方差分析无显著性意义。结论　天麻素在大鼠体内不存在肠肝循环更多还原

【Abstract】 OBJECTIVE To study the pharmacokinetics of gastr od in in rats.METHODS A permanent catheterization of jugular ve in as well as bile duct ligation method was applied and a reversed phase high p erformance liquid chromatographic method was established for the determination o f gastrodin in rat plasma.The data was processed with the software 3P87.RESULTS A good linearity was obtained from 25 μg·mL -1 to 800 μg·mL -1 of gastrodin with a correlation coefficient of 0.995.The detect ion limit was 20 μg·mL -1 .The extraction recovery was 83.6%.The RSD for t he intra day and inter day were less than 15%.The concentration time profile after iv administration was found to be fitted to a two compartment open model, but the concentration time curve after ig was fitted to a one compartment open model.The absolute bioavailability was 86.1%.The AUC of groups before and after bile duct ligation were (18±9) and (15±13) mg·min·mL -1 ,respectively.T here was no significant difference.CONCLUSION The finding su ggested that enterohepatic circulation of gastrodin did not exist in rats.更多还原