瑞巴派特分散片的人体药动学及生物等效性

发布时间：2018-02-03 21:53

本文关键词： 瑞巴派特液相色谱-串联质谱药动学生物等效性　出处：《中国医药工业杂志》2015年01期 　论文类型：期刊论文

【摘要】：建立了液相色谱-串联质谱法测定健康志愿者口服瑞巴派特分散片(受试制剂)和普通片(参比制剂,膜固思达~(?))后的血药浓度,估算两制剂的药动学参数并评价生物等效性。采用随机、开放、双周期交叉试验设计,22名男性健康志愿者单剂量口服受试或参比制剂0.1 g后,血样经乙腈直接沉淀蛋白后进行LC-MS/MS分析,利用DAS2.1.1软件计算药动学参数,并进行生物等效性评价。受试和参比制剂在人血浆中瑞巴派特的c_(max)为(236.9±l 03.4)和(233.9±105.1)ng/ml,t_(max)为(2.7±1.1)和(2.9±1.4)h,t_(1/2)为(2.0±0.8)和(2.3±1.5)h,AUC_(0→12h)为(929.0±291.9)和(970.5±353.2)ngh·ml~(-1)。受试制剂的相对生物利用度为(102.6±29.8)%。
[Abstract]:A liquid chromatography-tandem mass spectrometry (LC-MS) method has been established for the determination of oral repapet dispersible tablets (test preparations) and common tablets (reference preparation, membrane gustadine) in healthy volunteers. The pharmacokinetic parameters of the two preparations were estimated and bioequivalence was evaluated. A randomized, open, double-cycle cross-test design was used. 22 healthy male volunteers were given a single oral dose of 0.1 g or a reference preparation, and the blood samples were analyzed by LC-MS/MS after direct precipitation of protein by acetonitrile. The pharmacokinetic parameters were calculated by DAS2.1.1 software. The bioequivalence of the two preparations was 236.9 卤103.4) and 233.9 卤105.1 ng / ml in human plasma respectively. (2. 7 卤1. 1) and 2. 9 卤1. 4 hs (1 / 2), 2. 0 卤0. 8) and 2. 3 卤1. 5 hs respectively. 鈫扵he relative bioavailability of the tested preparations was 102.6 卤29.8, and 929.0 卤291.9) and 970.5 卤353.2ngh 路ml ~ (-1), respectively. You know...
【作者单位】：苏州大学附属第二医院临床药理实验室;
【分类号】：R969.1
【正文快照】： 瑞巴派特(rebamipide,1)由日本Otsuka公司开发生产,是一种前列腺素诱导剂,可以刺激前列腺素的产生;减弱中性粒细胞的活性,抑制细胞因子的产生,清除氧自由基。此外,还可以通过提高胃炥液中糖蛋白的含量、抑制胆汁酸,加强对胃炥膜的保护作用。临床用于治疗胃溃疡,改善急性胃炎

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