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一些用作抗菌治疗药物的喹诺酮类的光降解作用。

Photodegradation of some quinolones used as antimicrobial therapeutics.

作者信息

Tiefenbacher E M, Haen E, Przybilla B, Kurz H

机构信息

Walther-Straub Institute of Pharmacology and Toxicology, Ludwig-Maximilians-University, Munich, Germany.

出版信息

J Pharm Sci. 1994 Apr;83(4):463-7. doi: 10.1002/jps.2600830403.

DOI:10.1002/jps.2600830403
PMID:8046597
Abstract

The photostability of the fluoroquinolones ciprofloxacin (CPX), ofloxacin (OFX), and fleroxacin (FLX) toward ultraviolet irradiation (UVA) and room light was investigated in dilute aqueous solutions. A series of photoproducts was observed by high-performance liquid chromatography (HPLC) for all three drugs. As little as 1 h of exposure to room light was enough for the formation of detectable amounts of CPX photoproducts. The major CPX photoproduct was characterized as a dimer by liquid secondary ion mass spectrometry, but its structure was not determined. Since irradiation of CPX results (as cited in ref/11) in a loss of antibacterial activity and since all substances, parent drugs as well as their photoproducts, are potential candidates for undesired drug effects, quinolone drugs should be strictly protected from all light during storage and administration.

摘要

在稀水溶液中研究了氟喹诺酮类药物环丙沙星(CPX)、氧氟沙星(OFX)和氟罗沙星(FLX)对紫外线照射(UVA)和室内光的光稳定性。通过高效液相色谱法(HPLC)观察到这三种药物都产生了一系列光产物。暴露于室内光仅1小时就足以形成可检测量的CPX光产物。主要的CPX光产物通过液体二次离子质谱表征为二聚体,但其结构尚未确定。由于CPX照射(如参考文献11中所述)会导致抗菌活性丧失,并且所有物质,包括母体药物及其光产物,都可能产生不良药物效应,因此喹诺酮类药物在储存和给药期间应严格避光。

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Microbial transformations of antimicrobial quinolones and related drugs.抗菌喹诺酮类药物及相关药物的微生物转化。
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