【摘 要】
：
基于有机阳离了转运体(Organic cation transporters,rOCTs)和多药和毒素外排蛋白1(Multidrug and toxin extrusion protein 1,rMATE1)探究美托洛尔对二甲双胍药动学的影响.采用HPLC测定血浆、尿液和组织中二甲双胍,采用Western blotting评价OCTs和rMATE1的表达水平.单次或连续7天给药后,与二甲双胍组相比
【机 构】
：
兰州大学第一医院药剂科,甘肃兰州73000 兰州大学第一医院药剂科,甘肃兰州73000;兰州大学药
【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
基于有机阳离了转运体(Organic cation transporters,rOCTs)和多药和毒素外排蛋白1(Multidrug and toxin extrusion protein 1,rMATE1)探究美托洛尔对二甲双胍药动学的影响.采用HPLC测定血浆、尿液和组织中二甲双胍,采用Western blotting评价OCTs和rMATE1的表达水平.单次或连续7天给药后,与二甲双胍组相比,联合给药组二甲双胍血药浓度和AUC0→t显著降低,V/F显著增加(p＜0.05)；肝脏、肾脏和肌肉组织Kp显著增加(p＜0.01).连续7天给药后,与二甲双胍组相比,联合给药组肾脏rMATE1表达水平显著降低(p＜0.01),肝脏(rOCT1和rMATE1)和肾脏(rOCT1和rOCT2)表达水平无统计学差异(p＞0.05).单次给药后,与二甲双胍组相比,联合给药组二甲双胍尿排泄量显著增加(p＜0.01),而联合给药3、7、15、30和60天后,二甲双胍尿排泄量显著降低(p＜0.05).连续60天给药后,与二甲双胍组相比,联合给药组血浆LCA和尿酸水平显著增加(p＜0.01).美托洛尔增加二甲双胍肝脏、肾脏和肌肉组织的摄取,降低其血药浓度.多次联合给予美托洛尔后下调肾脏rMATE1的表达水平,降低二甲双胍尿排泄.此外,长期联合给药后能够增加大鼠血浆LCA和尿酸水平.
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