文献类型：期刊文章

作　　者：姚庆宇[1] 李健[1] 姚烨[1] 陈镕[1] 陈文君[1] 苏红[1] 杨亮[1] 薛钧升[1] 卢炜[2,1] 周田彦[2,1]

机构地区：[1]北京大学医学部药学院药剂学系,北京100191 [2]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：National Natural Science Foundation of China(NSFC,Grant No.81673500)

年　　份：2017

卷　　号：26

期　　号：6

起止页码：404-412

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 the current study, we established and validated a simple and sensitive liquid chromatography-tandem mass spectrometric method for the determination of 21-hydroxy deflazacort in nude mice plasma, and such a method was applied to a pharmacokinetic study. Using betamethasone as the internal standard, the plasma samples were pre-treated by precipitation with acetonitrile and then analyzed on a reversed-phase C18 column （50 mm×2 mm, 5 μm） with a mobile phase consisting of acetonitrile and 4.0 mM ammonium formate （pH was adjusted to 3.5 with formic acid （40：60, v/v））. The analyte was detected by a triple quadrupole tandem mass spectrometer using electrospray, and multiple reaction monitoring was employed to select 21-hydroxy deflazacort at m/z 400.2/124.0 and betamethasone at m/z 393.3/147.0 in the positive ion mode. The calibration curves were linear （r〉0.99） over the range of 0.5~,00 ng/mL. The intra- and inter-day precisions and accuracies were 4.5%-10.1% and -1.7%-10.7% respectively. This method was successfully applied to a preclinical administered with a single oral dose of 4 mg/kg deflazacort, and its pharmacokinetic study of deflazacort on female nude mice pharmacokinetics was characterized by a two-compartment model with first-order absorption.

关 键 词：DEFLAZACORT 21-Hydorxy deflazacort  LC-MS/MS Nude mice  PHARMACOKINETICS

分 类 号：R965]