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目的:考察柠檬苦素在大鼠体内的代谢途径,为阐明该药物的作用机制提供参考。方法:大鼠按80 mg·kg~(-1)灌胃给予柠檬苦素,收集胆汁、尿液和粪便,利用HPLC和LC-MS/MS测定大鼠胆汁、尿液和粪便中柠檬苦素的含量,计算其累积排泄量和累积排泄分数。结果:柠檬苦素在大鼠粪便、尿液和胆汁中的累积排泄分数合计约50%,只有近一半的药物以原型形式排泄出体外。原药从尿液和胆汁中的总排泄量<1%,大部分以原型药物通过粪便排出。结论:柠檬苦素在大鼠体内的主要排泄途径为粪便,少量药物吸收进入血液后通过肝脏代谢,少量药物通过尿液排出体外。
OBJECTIVE: To investigate the metabolic pathway of limonin in rats and to provide reference for elucidating the mechanism of action of limonin. METHODS: Limonin was administered intragastrically to rats at a dose of 80 mg · kg -1. Bile, urine and feces were collected. The contents of limonin in rat bile, urine and feces were determined by HPLC and LC-MS / MS Content, calculate its cumulative excretion and cumulative excretion fraction. Results: The cumulative excretion of limonin in rat feces, urine and bile was about 50%. Only about half of the drugs were excreted in the form of prototypes. The original drug from the urine and bile in the total excretion <1%, most of the prototype drugs excreted through the feces. Conclusion: The main excretion pathway of limonin in rats is stool. A small amount of drug is absorbed into the blood and metabolized by the liver, and a small amount of drug is excreted through the urine.