文献类型：期刊文章

作　　者：从双晨[1] 张媛媛[1] 雷冏茜[1] 宋茂远[1] 张文茜[1] 彭光华[1] 殷梦雅[1] 李佳佳[1] 王佳星[1] 李馨儒[1]

机构地区：[1]北京大学医学部药学院分子药剂学与新释药系统北京市重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》

基　　金：The National Basic Research Program of China(Grant No.2015CB932100)

年　　份：2017

卷　　号：26

期　　号：8

起止页码：589-594

语　　种：中文

收录情况：CAB、CAS、CSCD、CSCD2017_2018、DOAJ、EMBASE、IC、JST、SCOPUS、ZGKJHX、普通刊

摘　　要：In this study, a sensitive and rapid LC-MS/MS method was developed and validated to determine dabigatran in plasma of beagle dogs after oral administration of dabigatran etexilate nanosuspension （DABE-NS）. The analytes （dabigatran） and sertraline hydrochloride （internal standard, IS） were separated on a Kromasil C18 column using gradient elution consisting of methanol and formate buffer at a flow rate of 0.4 mL/min in 20 min. Detection and quantitation were carded out by multiple reaction monitoring following the transitions： m/z 472.17→289.07 and 305.98→275.00 for dabigatran and IS at positive ion mode, respectively. The calibration curves were linear from 1.0 to 500.0 ng/mL for dabigatran with r = 0.9995. The accuracy of each analyte ranged from 94.8% to 107.1%, and the precision was within 6%. Besides, this method was successfully applied in the investigation of the pharmacokinetic profile of dabigatran in beagle dogs after oral administration of DABE-NS. The maximum concentration and the areas under curves of dabigatran for DABE-NS were significantly higher than those of control formulation, indicating improved oral absorption.

关 键 词：DABIGATRAN Dabigatran etexilate  LC-MS/MS NANOSUSPENSION PHARMACOKINETICS

分 类 号：O657.72] R965[化学类]