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[抗真菌药的光稳定性。3. 局部作用抗真菌药的光稳定性]

[The photostability of antimycotics. 3. Photostability of locally acting antimycotics].

作者信息

Thoma K, Kübler N, Reimann E

机构信息

Institut für Pharmazie und Lebensmittelchemie, Ludwig-Maximilians-Universität, München, Germany.

出版信息

Pharmazie. 1997 May;52(5):362-73.

PMID:9229718
Abstract

The photochemical stability of a number of topical antimycotic drugs was tested. The light sensitivity decreases in the order naftifine, sulbentine, cloxiquin, tolnaftate and chlorphenesin. A liquid chromatography-mass spectrometry system was used to identify a number of photodegradation products. Light exposure of sulbentine leads to the formation of benzylisothiocyanate. Chlorphenesine solutions undergo photodehalogenation with the formation of varying photodegradation products depending on the solvent used. The photochemical reactions of naftifine are a cis-trans-isomerization and the formation of a dimer product. Drug preparations are also degraded under light exposure in a simulated topical application. Excipients in the drug preparations strongly influence the photodegradation kinetics and the chemical structure of photodegradation products.

摘要

测试了多种局部抗真菌药物的光化学稳定性。光敏感性按萘替芬、舒布替林、氯碘喹啉、托萘酯和氯苯甘醚的顺序降低。使用液相色谱 - 质谱系统鉴定了多种光降解产物。舒布替林光照会导致异硫氰酸苄酯的形成。氯苯甘醚溶液会发生光脱卤反应,根据所用溶剂的不同会形成不同的光降解产物。萘替芬的光化学反应是顺反异构化以及二聚体产物的形成。药物制剂在模拟局部应用的光照下也会降解。药物制剂中的辅料强烈影响光降解动力学和光降解产物的化学结构。

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