醋柴胡小分子水溶性部位对甲氨蝶呤药物代谢动力学的影响

发布时间：2018-11-12 11:36

【摘要】：目的:探讨P-糖蛋白抑制剂醋柴胡小分子水溶性部位(MHE)对甲氨蝶呤药动学行为的影响。方法:SD雄性大鼠分别灌胃甲氨蝶呤或甲氨蝶呤联合MHE后,于不同时间点眼眶静脉丛采血,利用20%高氯酸沉淀蛋白法处理血样,采用高效液相色谱法分析,非隔室模型估算药代动力学参数。结果:与单用组比较,联用组甲氨蝶蛉药时曲线下面积AUC0-t增加16.6%,AUC0-∞增加33.8%,生物半衰期(t1/2)延长了1.2倍,平均驻留时间(MRT0-t)增加了26.1%,而药物清除率(CL)下降了20.3%,但2组的药代动力学参数无显著性差异。结论:MHE具有增强甲氨蝶呤生物利用度的趋势,二者联合用药需要关注毒副反应的发生。
[Abstract]:Aim: to investigate the effect of water soluble fraction (MHE) on the pharmacokinetics of methotrexate (MTX). Methods: after intragastric administration of methotrexate or methotrexate combined with MHE, blood samples were collected from orbital venous plexus at different time points in SD male rats. The blood samples were treated by 20% perchloric acid precipitation protein method and analyzed by high performance liquid chromatography (HPLC). The pharmacokinetic parameters were estimated by non compartment model. Results: compared with the single group, the area under the curve (AUC0-t) increased by 16.6%, AUC0- 鈭，

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