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Repaglinide

内分泌

关键词内分泌 治疗药物 糖尿病

词汇介绍

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解析

Repaglinide

释    义   瑞格列奈

例    句   Objective: To observe the clinical efficacy and safety of combined treatment of repaglinide and acarbose in aged patients with diabetes type 2. 目的:观察瑞格列奈、阿卡波糖联合治疗老年性2型糖尿病患者的临床疗效及安全性。

概述

瑞格列奈是一种抗糖尿病药,称为美格替尼,于1983年发明,瑞格列奈是一种口服药物,除饮食和运动外,可用于控制2型糖尿病的血糖。瑞格列奈的作用机制涉及促进胰腺β胰岛细胞释放胰岛素。像其他抗糖尿病药一样,主要的副作用是低血糖症。机制瑞格列奈可通过刺激胰腺β胰岛细胞释放胰岛素来降低血糖,它通过关闭β细胞膜中ATP依赖性钾离子通道来实现,这使β细胞去极化,打开细胞的钙通道,并且所产生的钙内流诱导胰岛素分泌。吸收:瑞格列奈从胃肠道吸收时具有56%的生物利用度。与食物一起服用会降低生物利用度,最大浓度降

Pharmacokinetic Evaluation of Metabolic Drug Interactions between Repaglinide and Celecoxib by a Bioanalytical HPLC Method for Their Simultaneous Determination with Fluorescence Detection复制标题

瑞格列奈与塞来昔布代谢药物相互作用的药代动力学评价生物分析HPLC法同时荧光检测

发表时间:2019-08-02

影响因子:4.8

作者: Dong-Gyun Han

期刊:Pharmaceutics

Arthritis and diabetes mellitus are highly prevalent diseases with a total of over 350 million patients worldwide. The most common types of arthritis and diabetes mellitus are osteoarthritis (OA) and type 2 diabetes mellitus (T2DM), respectively. OA affects 14% of adults aged ≥25 years, and 34% of these patients are aged >65 years; similarly, T2DM affects 12% of adults aged ≥20 years, and 26% of these are aged >65 years. A recent survey estimated that the prevalence of OA was higher in individuals with T2DM than in those without T2DM. Thus, T2DM is generally recognized as a comorbidity of arthritis, while some previous studies have focused on diabetes as a risk factor of arthritis. Anyway, it is evident that T2DM is closely associated with an increased incidence and prevalence of OA, though the reasons remain unclear.Because T2DM frequently co-exists with OA, there is a possibility of concurrent administration of REP and CEL. Hence, a bioanalytical method of simultaneous determination of REP and CEL could be useful and efficient for further pharmaceutical development and therapeutic optimization. To date, several bioanalytical methods have been developed and validated for quantitative determination of REP or CEL individually using HPLC with UV/Vis detection or using liquid chromatography with tandem mass spectrometry (LC-MS/MS) systems. However, these methods are associated with a few limitations, such as an insufficient sensitivity, relatively large sample volume, and/or time-consuming liquid–liquid extraction procedures with volatile solvents that are potentially hazardous to health. Moreover, LC-MS/MS methods require relatively complex and/or expensive instrumentation, which may not be affordable for small-sized laboratories and companies in resource-limited settings. To the best of our knowledge, there have been no reported methods of simultaneous quantification of REP and CEL in biological samples using HPLC coupled with a fluorescence detector (HPLC-FL). Furthermore, a previous in vitro study reported that CEL inhibited REP metabolism in pooled human liver microsomes (HLM) with a Ki of 3.1 μM. This suggests the possibility of pharmacokinetic drug interaction between REP and CEL, but no information is currently available regarding this issue.

译文

关节炎和糖尿病是高度流行的疾病,全世界共有超过3.5亿患者。关节炎和糖尿病最常见的类型分别是骨关节炎(oa)和2型糖尿病(t2dm)。oa影响14%的年龄≥25岁的成年人,34%的患者年龄>65岁;同样,t2dm影响12%的年龄≥20岁的成年人,26%的患者年龄>65岁。最近的一项调查估计,患有2型糖尿病的人oa的患病率高于没有患有2型糖尿病的人。因此,人们普遍认为2型糖尿病是关节炎的一种共病,而以前的一些研究则把糖尿病作为关节炎的危险因素。无论如何,很明显,2型糖尿病与oa发病率和患病率的增加密切相关,尽管原因尚不清楚。由于T2DM经常与OA共存,有可能同时给予ReP和CEL。因此,一种同时测定rep和cel的生物分析方法可以为进一步的药物开发和治疗优化提供有效的手段。迄今为止,已经开发了几种生物分析方法,并通过紫外/可见检测高效液相色谱法或串联质谱(lc-ms/ms)系统分别对rep或cel进行了定量测定。然而,这些方法有一些局限性,例如灵敏度不足、相对较大的样品体积和/或使用可能危害健康的挥发性溶剂的耗时的液-液萃取程序。此外,LC-MS/MS方法需要相对复杂和/或昂贵的仪器,在资源有限的环境中,小型实验室和公司可能负担不起。据我们所知,目前还没有使用高效液相色谱-荧光检测器(hplc-fl)同时定量生物样品中rep和cel的方法。此外,先前的一项体外研究报告称,cel以3.1μm的ki抑制了人肝微粒体(hlm)中rep的代谢。这表明rep和cel之间可能存在药代动力学药物相互作用,但目前还没有这方面的信息。