天麻素在大鼠体内的药动学研究

Pharmacokinetics of gastrodin in rats

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。

OBJECTIVE: To study the pharmacokinetics of gastrodin in rats. METHODS: A permanent catheterization of jugular vein as well as bile duct ligation method was applied and a reversed phase high-performance liquid chromatographic method was established for the determination of gastrodin in rat plasma. The data was processed with the software 3P87. RESULTS: A good linearity was obtained from 25 μg&middotmL-1 to 800μg&middotmL-1 of gastrodin with a correlation coefficient of 0.995. The detection limit was 20 μg&middot mL-1. The extraction recovery was 83.6%. The RSD for the 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&middotmin&middotmL-1, respectively. There was no significant difference. CONCLUSION: The finding suggested that enterohepatic circulation of gastrodin did not exist in rats.