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氟喹诺酮是一类广泛用于临床的抗菌化疗药物。近年来,新氟喹诺酮的研发日新月异,迄今已有7000多个类似物被合成。以外消旋体、非对映异构体或纯对映体存在的不同氟喹诺酮(FQ)的结构中含有1个或2个手性中心。在临床应用和药学领域,必须建立一套行之有效的分析程序对氟喹诺酮进行质量控制以及药动学和药效学的研究。本文重点讨论了利用衍生法和配位体交换(LE)或手性液相色谱等技术对氟喹诺酮对映体进行高效液相色谱(HPLC)分离的方法。
Fluoroquinolones are a class of antibacterial chemotherapeutic drugs that are widely used in clinical practice. In recent years, the research and development of new fluoroquinolones are rapidly changing, and so far more than 7000 analogues have been synthesized. Different fluoroquinolones (FQs), which exist as racemates, diastereomers or as pure enantiomers, contain one or two chiral centers in their structure. In the field of clinical application and pharmacy, it is necessary to establish a set of effective analytical procedures for the quality control of fluoroquinolones and the study of pharmacokinetics and pharmacodynamics. This article focuses on the separation of fluoroquinolone enantiomers by high performance liquid chromatography (HPLC) using derivatization and ligand exchange (LE) or chiral liquid chromatography techniques.