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新型抗肿瘤药物LS-177在大鼠体内的排泄研究

Excretion of a Novel Anticancer LS-177 in Rats

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【作者】 张伦会刘珍珍陈晓辉刘亿

【Author】 ZHANG Lun-hui;LIU Zhen-zhen;CHEN Xiao-hui;LIU Yi;The Affiliated Hospital of Southwest Medical University,Department of Pharmacy;Medical School of Yangtze University;Shenyang Pharmaceutical University;The Affiliated Hospital of Southwest Medical University,Department of Gastrointestinal Surgery;

【机构】 西南医科大学附属医院药学部长江大学医学院沈阳药科大学西南医科大学附属医院胃肠外科

【摘要】 目的研究LS-177在大鼠体内的排泄情况。方法建立快速、灵敏的UPLC-MS/MS分析方法测定单次灌胃给予50.0mg·kg-1的LS-177混悬液后,LS-177原型药物自雄雌大鼠尿液、胆汁和粪便中的排泄量。结果大鼠灌胃给药后,尿液96 h内、胆汁24 h内的累积排泄百分率具有明显的雌雄差异(P<0.05),粪便96 h内的雌雄差异不明显(P>0.05)。结论原型药物在尿液、胆汁和粪便中总的回收量约占给药剂量的50%,其中主要是由粪便排出体外,推测LS-177口服吸收差是其生物利用度低的主要原因。

【Abstract】 OBJECTIVE To study the excretion profile of LS-177 in rats. METHODS A selective,sensitive and accurate UPLC-MS/MS assay was developed and validated for the determination of LS-177 in rat urine,bile and feces. RESULTS After oral administration of LS-177 oral suspension at the dose of 50 mg·kg-1,there was significant difference in the excretion percentages of LS-177 between male and female rats both in urine and bile. No significant difference was observed in the excretion of LS-177 through feces. CONCLUSION The data suggests that unabsorbed LS-177 excretion in feces is the main excretion pathway,indicating that poor oral absorption is the main cause of low bioavailability.

【关键词】 LS-177液相色谱质谱联用法排泄尿液粪便胆汁肿瘤
【Key words】 LS-177UPLC-MS/MSexcretionurinefecesbilecancer
  • 【文献出处】 中国药学杂志 ,Chinese Pharmaceutical Journal , 编辑部邮箱 ,2018年02期
  • 【分类号】R965
  • 【被引频次】2
  • 【下载频次】309
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