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本文用反相高效液相色谱法研究了天麻素在大鼠体内的生理处置。于大鼠在体肠袢注入天麻素后15及30min 分别回收给药剂量的66%和47.4%天麻素静注后2min 组织内药物分布以肾脏含量最高。本品不能通过血脑屏障进入脑内,但其代谢产物对羟基苯甲醇(甙元)在脑组织中可被检出。天麻素血浆蛋白结合率为7.8%。组织温孵实验表明,天麻素在全血、肺、肝和肾组织中的回收率分别为99.1%、99.8%、91.2%和47.68%。体外肾切片温孵可使天麻素转化为其甙元。天麻素主要以原形药的形式从尿中排泄,胆汁中排出甚微,娄便中未检出原形药及其甙元。
In this paper, the physiological treatment of gastrodin in rats was studied by RP-HPLC. After the gastroenteral injection of gastrodin in rats at 15 and 30 min, 66% of the doses and 47.4% of gastrodins were injected intramuscularly, respectively. The distribution of the drugs in the tissues was the highest in the kidneys. This product can not enter the brain through the blood-brain barrier, but its metabolite p-hydroxybenzyl alcohol (a glycoside) can be detected in brain tissue. Gastrodin plasma protein binding rate was 7.8%. Tissue incubation experiments showed that the recovery of gastrodin in whole blood, lung, liver and kidney tissues was 99.1%, 99.8%, 91.2% and 47.68%, respectively. In vitro kidney section incubation can convert gastrodin to its aglycone. Gastrodin is mainly excreted in the urine in the form of original drugs, and bile discharge is minimal. The prototype drug and its aglycone are not detected in the stool.