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0.3%环丙沙星、0.3%氧氟沙星和0.5%莫西沙星在摘除的人眼中角膜和房水的渗透情况。

Penetration of 0.3% ciprofloxacin, 0.3% ofloxacin, and 0.5% moxifloxacin into the cornea and aqueous humor of enucleated human eyes.

作者信息

Silva G C M, Jabor V A P, Bonato P S, Martinez E Z, Faria-E-Sousa S J

机构信息

Departamento de Oftalmologia, Faculdade de Medicina de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brasil.

Departamento de Física e Química, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brasil.

出版信息

Braz J Med Biol Res. 2017 Jul 3;50(7):e5901. doi: 10.1590/1414-431X20175901.

Abstract

We aimed to quantify the penetration of ciprofloxacin, ofloxacin, and moxifloxacin into the cornea and aqueous humor of cadaver eyes. A total of 60 enucleated eyes, not eligible for corneal transplantation, were divided into three groups and immersed in commercial solutions of 0.3% ciprofloxacin, 0.3% ofloxacin, or 0.5% moxifloxacin for 10 min. Whole corneas and samples of aqueous humor were then harvested and frozen, and drug concentrations analyzed by liquid chromatography tandem mass spectrometry. The mean corneal concentration of moxifloxacin was twice as high as ofloxacin, and the latter was twice as high as ciprofloxacin. The mean concentration of moxifloxacin in the aqueous humor was four times higher than the other antibiotics, and the mean concentrations of ciprofloxacin and ofloxacin were statistically similar. The amount of drug that penetrated the anterior chamber after a 10-min immersion was far below the safe limit of endothelial toxicity of each preparation. Moxifloxacin demonstrated far superior penetration into the cornea and anterior chamber of cadaver eyes compared to ciprofloxacin and ofloxacin. One should not expect endothelial toxicity with the commercial eye drops of ciprofloxacin, ofloxacin, and moxifloxacin that reach the anterior chamber through the cornea.

摘要

我们旨在量化环丙沙星、氧氟沙星和莫西沙星在尸体眼的角膜和房水中的渗透情况。总共60只不符合角膜移植条件的摘除眼球被分为三组,并浸入0.3%环丙沙星、0.3%氧氟沙星或0.5%莫西沙星的市售溶液中10分钟。然后采集整个角膜和房水样本并冷冻,通过液相色谱串联质谱法分析药物浓度。莫西沙星的平均角膜浓度是氧氟沙星的两倍,而后者是环丙沙星的两倍。莫西沙星在房水中的平均浓度比其他抗生素高四倍,环丙沙星和氧氟沙星的平均浓度在统计学上相似。浸泡10分钟后穿透前房的药物量远低于每种制剂内皮毒性的安全限度。与环丙沙星和氧氟沙星相比,莫西沙星在尸体眼的角膜和前房中的渗透能力要强得多。对于通过角膜到达前房的环丙沙星、氧氟沙星和莫西沙星市售滴眼液,不应预期会出现内皮毒性。

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