沙坦类药物的质谱裂解规律及其应用  

Mass Fragmentation Patterns of Sartans and Application

作　　者：蔡鹏俊[1] 李悦[1] 

机构地区：[1]中国医药工业研究总院上海医药工业研究院创新药物与制药工艺国家重点实验室,上海201203

出　　处：《中国医药工业杂志》2017年第1期68-77,共10页Chinese Journal of Pharmaceuticals

摘　　要：为探索一种利用质谱快速鉴定血管紧张素Ⅱ受体拮抗药中未知杂质结构的方法,采用电子轰击质谱(EI-MS)和电喷雾串联质谱(ESI-MS/MS)研究已上市的6种沙坦类药物。通过解析碎片离子并结合高分辨质谱确证裂解途径,总结沙坦类药物的质谱裂解规律,并将其应用于未知杂质结构的快速鉴定。据此鉴定了阿齐沙坦原料药中的2个未知的同分异构体杂质,杂质1为噁二唑环的氮原子被乙基化,杂质2为阿齐沙坦羧酸乙酯。Six listed sartan drugs were studied by electron impact ionization-mass spectrometry （EI-MS） and electrospray ionization-tandem mass spectrometry （ESI-MS/MS） in order to explore a rapid method for the identification of unknown impurities in angiotensin II receptor blockers. Through the analysis of the main fragment ions and the data of high resolution mass spectrometry, fragmentation patterns and regularities were summarized and utilized in the rapid identification of unknown impurities. The structures of two unknown enantiomeric impurities in azilsartan were identified based on the above findings, impurity 1 was the ethylated product on nitrogen of oxadizole and impurity 2 was the ethyl ester of azilsartan.

关 键 词：沙坦类药物 电子轰击电离 电喷雾电离 质谱 裂解规律 结构鉴定 

分 类 号：O657.63[理学—分析化学]