Beagle犬血浆中达比加群的UPLC-MS/MS法测定  

Determination of Dabigatran in Beagle Dog Plasma by UPLC-MS/MS

作　　者：向志雄[1] 马文狄[1] 夏广新[1] 

机构地区：[1]上海医药集团股份有限公司中央研究院,上海201203

出　　处：《中国医药工业杂志》2015年第10期1096-1099,共4页Chinese Journal of Pharmaceuticals

摘　　要：建立了超高效液相色谱-串联质谱法测定Beagle犬血浆中的达比加群。以达比加群-d3为内标,使用BEH C18色谱柱,采用ESI离子源,多反应监测（MRM）模式进行正离子检测。达比加群的线性范围为1~1 000 ng/ml。日内、日间RSD均小于15%。同时测定了服用甲磺酸达比加群酯胶囊后Beagle犬的血药浓度,其主要药动学参数分别为：tmax（1.8±0.3）h,cmax（113.8±65.0）ng·ml-1,AUC0→t（657.4±340.8）ng·h·ml-1,AUC0→∞（716.5±397.8）ng·h·ml-1,MRT（8.7±2.2）h,t1/2（5.9±1.9）h。A UPLC-MS/MS method was established for the determination of dabigatran in Beagle dog plasma. Dabigatran-d3 was chosen as the internal standard. A BEH C18 column was used, with the application of ESI ion source, in the positive ion mode, combined with multiple reaction monitoring （MRM） mode. It was linear in the range of 1 - 1 000 ng/ml. The intra- and inter-day RSDs were less than 15 %. The drug concentration of dabigatran in Beagle dog plasma was determined, and the main pharmacokinetic parameters of dabigatran etexilate mesylate after oral administration to Beagle dogs were as follows： tmax （1.8±0.3） h, Cmax （113.8±65.0） ng·ml^-1, AUC0→t （657.4± 340.8） ng·h·ml^-1, AUC0→∞ （716.5±397.8） ng·h·ml^-1. MRT （8.7±2.2）h. t1/2 （5.9±1.9） b.

关 键 词：达比加群 超高效液相色谱-串联质谱 药动学 测定 

分 类 号：R969[医药卫生—药理学] O657.72[医药卫生—药学]