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目的:分析大鼠灌胃刺五加提取物后血浆、胆汁、尿液和粪便中异嗪皮啶(M0)及其代谢产物。方法:健康雄性wistar大鼠按325 mg.kg-1的剂量灌胃给予刺五加提取物,分别采集给药后1,1.5,2,4,6 h肝门静脉血液并用SPE技术制备血浆;采集0～12 h胆汁并用SPE技术制备;0～12 h,12～24 h分别采集尿液和粪便样品并制备样品,采用UPLC-Q-TOF-MS技术和Metabolynx XS软件联合的方法分析。结果:在大鼠血浆、胆汁、尿液和粪便中检测到M0,在血浆和胆汁中检测到代谢物异嗪皮啶葡萄糖醛酸苷(M1)。其中M1是首次报道的异嗪皮啶代谢产物。结论:异嗪皮啶在大鼠体内以葡萄糖醛酸形式代谢,最终又以异嗪皮啶形式排出体外。
OBJECTIVE: To analyze isoxapine (M0) and its metabolites in plasma, bile, urine and feces of rats after acanthopanax senticosus extract. METHODS: Healthy male wistar rats were given gavage of Acanthopanax senticosus at a dose of 325 mg.kg-1. The hepatic portal vein blood was collected at 1, 1.5, 2, 4 and 6 h after administration and plasma was prepared by SPE technique. 0 ~ 12 h bile was prepared by SPE technique. Urine and stool samples were collected at 0-12 h and 12-24 h, respectively. Samples were prepared and analyzed by UPLC-Q-TOF-MS and Metabolynx XS software. Results: M0 was detected in rat plasma, bile, urine and feces, and the metabolite isracalidin glucuronide (M1) was detected in plasma and bile. Among them, M1 was the first reported isclizidine metabolite. Conclusion: Isoxabine is metabolized in the form of glucuronic acid in rats and finally excreted in the form of isopyrazid.