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苄达明的光降解:一种分离出的光产物对红细胞的光毒性。

Photodegradation of benzydamine: phototoxicity of an isolated photoproduct on erythrocytes.

作者信息

Vargas F, Rivas C, Machado R, Sarabia Z

机构信息

Centro de Química, Instituto Venezolano de Investigaciones Científicas I.V.I.C., Caracas, Venezuela.

出版信息

J Pharm Sci. 1993 Apr;82(4):371-2. doi: 10.1002/jps.2600820407.

DOI:10.1002/jps.2600820407
PMID:8468680
Abstract

Benzydamine hydrochloride (Tantum, 1) is a photoallergic and phototoxic anti-inflammatory and analgesic agent. This drug is photolabile under aerobic and anaerobic conditions. Irradiation of a methanol solution of benzydamine under oxygen or argon at 300 nm affords 5-hydroxybenzydamine (2) and 2-beta-dimethylaminopropyl-1-benzylindalolin-3-one (3) as the main isolated and spectroscopically identified photoproducts. A radical intermediate was evidenced by thiobarbituric acid that was used as a radical sonde, as well as by the dimerization of cysteine. Erythrocyte lysis photosensitized by 1, 2, and 3 was investigated.

摘要

盐酸苄达明(坦通,1)是一种具有光过敏和光毒性的抗炎镇痛药。该药物在有氧和无氧条件下均具有光敏感性。在氧气或氩气存在下,用300 nm波长的光照射苄达明的甲醇溶液,主要分离得到并经光谱鉴定的光产物为5-羟基苄达明(2)和2-β-二甲基氨基丙基-1-苄基吲哚啉-3-酮(3)。用硫代巴比妥酸作为自由基探测器以及通过半胱氨酸的二聚化证明了存在自由基中间体。研究了1、2和3对红细胞裂解的光敏作用。

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