【摘 要】
：
溃疡性结肠炎(UC)状态下体内一些代谢酶的功能与表达会发生改变,且近期有报道使用质子泵抑制剂奥美拉唑(OME)治疗溃疡性结肠炎(UC),因此本研究考察OME在UC模型大鼠不同病期肝、肾、肠微粒体中奥美拉唑代谢酶活性的变化.给予大鼠自由饮用5％葡聚糖硫酸钠(DSS)7天诱导急性期UC(UCA)大鼠模型,7天DSS后改正常饮水7天诱导恢复期UC(UCR)大鼠模型.同时制备UCA、UCR以及正常对照(N
【机 构】
：
常州市第一人民医院药剂科,常州,江苏 中华医药研究院,澳门大学,澳门
【出 处】
：
2015第11届全国药物和化学异物代谢学术会议
论文部分内容阅读
溃疡性结肠炎(UC)状态下体内一些代谢酶的功能与表达会发生改变,且近期有报道使用质子泵抑制剂奥美拉唑(OME)治疗溃疡性结肠炎(UC),因此本研究考察OME在UC模型大鼠不同病期肝、肾、肠微粒体中奥美拉唑代谢酶活性的变化.给予大鼠自由饮用5％葡聚糖硫酸钠(DSS)7天诱导急性期UC(UCA)大鼠模型,7天DSS后改正常饮水7天诱导恢复期UC(UCR)大鼠模型.同时制备UCA、UCR以及正常对照(NOR)组大鼠的肝、肾、肠微粒体.将不同浓度的OME与各微粒体共孵育,通过LC/MS/MS检测样品中5-OH OME的生成量,比较OME在各组微粒体中的代谢活性.连续饮用5％ DSS7天,UCA和UCR组大鼠表现出明显的结肠炎症状.DSS停药七天后,UCR组大鼠症状有所好转.UCA组肝微粒体中5-OH OME的生成速率显著高于正常组,UCA组的CLint与NOR组相比降低了45％,而UCR组的生成速率可恢复到正常水平.OME在大鼠肾微粒体中的代谢表现为二相代谢.OME在三组大鼠肾和肠微粒体中的代谢活性均无显著差异.结果表明OME在肝微粒中的代谢会受到UC疾病和病程的影响而改变,可能会影响到OME在患者体内的药物代谢动力学.
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