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非布司他降解产物的LC-MS研究
引用本文:冷柏榕, 严相平, 王康蕊, 王德才. 非布司他降解产物的LC-MS研究[J]. 中国现代应用药学, 2012, 29(3): 226-229.
作者姓名:冷柏榕  严相平  王康蕊  王德才
作者单位:1.南京工业大学江苏省药物研究所,南京 210009;2南京工业大学药学院,南京 211816
摘    要:
目的 研究非布司他的降解产物。方法 强制降解后以LC-MS测定,根据质谱测定结果结合结构及反应机制推测降解产物结构。结果 推测降解产物为2-[3-氰基-4-(2-异丁氧基)苯基]-4-甲基噻唑-5-羧酸甲酯、2-[3-氨基甲酰基-4(2-异丁氧基-)苯基]-4-甲基噻唑-5-羧酸、2-[3-氰基-4-(2-异丁氧基)苯基]-4-甲基-1-氧化噻唑-5-羧酸甲酯以及非布司他的二聚体。结论 该法为研究非布司他的稳定性及其可能的降解途径提供了参考。

关 键 词:非布司他  液相色谱-质谱  有关物质  降解产物
收稿时间:2011-08-01
修稿时间:2011-11-30

Study on Degradation Products of Febuxostat by LC-MS
LENG Borong, YAN Xiangping, WANG Kangrui, WANG Decai. Study on Degradation Products of Febuxostat by LC-MS[J]. Chinese Journal of Modern Applied Pharmacy, 2012, 29(3): 226-229.
Authors:LENG Borong  YAN Xiangping  WANG Kangrui  WANG Decai
Affiliation:1.Jiangsu Provincial Institute of Material Medica, Nanjing University of Technology, Nanjing 210009, China; 2.School of Pharmaceutical Sciences, Nanjing University of Technology, Nanjing 211816, China
Abstract:
OBJECTIVE To investigate the degradation products of febuxostat. METHODS After forced degradation, products were determined by LC-MS. The structures of degradation products were elucidated by the results of mass spectrometry combined with the structure and the reaction mechanism. RESULTS It was speculated that the degradation products were 2-(3-cyano-4-isobutoxy-phenyl)-4-methyl-thiazole-5-carboxylic acid methyl ester, 2-(3-carbamoyl-4-isobutoxyphenyl)-4- methylthiazole-5-carboxylic acid, 2-(3-cyano-4-isobutoxy-phenyl)-4-methyl-1-oxidation thiazole -5-carboxylic acid methyl ester, a dimmer of febuxostat. CONCLUSION The method provides a reference of studying the stability of febuxostat and possible degradation pathway.
Keywords:febuxostat   LC-MS   related substance   degradation product
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