盐酸安舒法辛临床前吸收药物代谢动力学及脑内分布研究

发布时间：2018-06-27 14:20

本文选题：安舒法辛 + ODV　；参考：《吉林大学》2014年硕士论文

【摘要】：安舒法辛是ODV（ODV）的酯化前药，在体内经酯酶水解后转化为活性产物ODV，属于5-羟色胺-去甲肾上腺素重摄取抑制剂（SNRI）型抗抑郁药，具有组织突出前细胞受体作用功能，致使体液中5-羟色胺和去甲肾上腺素浓度升高的药理活性。本研究建立了适用于测定Wistar大鼠血浆、脑组织以及下丘脑组织中安舒法辛和ODV含量的LC-MS/MS分析方法，以此对盐酸安舒法辛在大鼠体内的吸收药动学和脑组织分布特征进行了考察，并与ODV的此方面特征进行了对比和分析。利用DAS3.0、SPSS13.0等软件对药代参数进行了计算并对结果进行了统计学分析；同时对两种药物在体内靶向位点—脑部的分布情况进行了比较和分析。本研究开发了快速、灵敏、准确的分析方法，，为安舒法辛在临床上的应用提供了必要的参考数据。
[Abstract]:Amsufaxine is a pre-esterification drug of ODV, which is transformed into the active product ODV by esterase hydrolysis in vivo. It belongs to serotonin norepinephrine reuptake inhibitor (SNRI) type antidepressant, and has the function of tissue protruding precellular receptor. The pharmacological activity that results in increased concentrations of serotonin and norepinephrine in body fluids. In this study, a LC-MS / MS analysis method was established for the determination of ambrofacin and ODV in plasma, brain and hypothalamus of Wistar rats. The absorption pharmacokinetics and brain tissue distribution of amsufacin hydrochloride in rats were investigated. And the characteristics of ODV are compared and analyzed. The pharmacokinetic parameters were calculated by DAS3.0 and SPSS 13.0 software, and the results were statistically analyzed, and the distribution of the two drugs in the brain targeting sites in vivo was compared and analyzed. In this study, a rapid, sensitive and accurate analytical method has been developed, which provides the necessary reference data for the clinical application of ambrofacin.
【学位授予单位】：吉林大学
【学位级别】：硕士
【学位授予年份】：2014
【分类号】：R969.1

【参考文献】