7-氨噻肟头孢菌素的聚合物分析

Analysis of polymers of cephalosporins with an aminothiazoyl ring at the C-7 position

在头孢菌素类药物杂质谱的控制中,对聚合物类杂质的分析是其最薄弱环节。7-氨噻肟头孢菌素是第三代头孢菌素的典型代表,也是当前仿制药一致性评价的热点品种。本文通过回顾近年来对7-氨噻肟头孢菌素聚合物分析取得的进展,归纳总结该类头孢菌素的聚合反应特性、聚合物特性和常见的聚合物衍生物/降解物,试图解决LC-MS分析聚合物结构中的常见困惑,形成对该类抗生素聚合物分析相对系统的策略与方法。

Analysis of polymer impurities of cephalosporins is the weakest link in the impurity profiling.Cephalosporins with an aminothiazoyl ring at the C-7 position are a typical representative of the third-generation ones,and the popular antibiotics in the generic consistency evaluation at present. In this paper, by reviewing the progress of analysis on polymers in recent years, we summaries the characteristics of polymerization reaction, the properties of polymers, and some common polymerization derivatives/degradators on these kinds of cephalosporins, and attempts to solve some confusion met in the polymer structure analysis by LC-MS. Finally, we hope to form a systematic strategy and find suitable methods for the analysis of these polymers.