Portolés M, Igual A, Jauch A, Nos-Barbéra S
Laboratorios cusi, Barcelona, Spain.
Lens Eye Toxic Res. 1990;7(3-4):469-80.
Lomefloxacin (NY-198) is a chemotherapic agent from the new 4-quinolone group, acting on DNA gyrase system. Lomefloxacin (LFLX), as some other new 4-quinolone compounds are antimicrobials of potential use for ophthalmic application. A first approach on the oculotoxicity of LFLX is the main purpose of this study. Four concentrations of LFLX (10, 30, 100 and 300 micrograms/ml) were tested on the first subculture of pigmented rabbit corneal epithelial cells. Cell number, protein contents, neutral red stain and wound healing were evaluated. The results showed that the lower concentrations (10 & 30 micrograms/ml) had no effect while the highest one had a remarkable cytotoxic effect. Pharmacokinetic data show that peak values achieved in the cornea and other ocular structures are lower than 40 micrograms/g (0.3% topical application) and, on another hand, MIC values range from less than or equal to 0.05 to 16 micrograms/ml. So, these "critical" concentrations have no cytotoxic effects according to our results. Then, it is concluded that Lomefloxacin could be a useful drug for topical ophthalmic development.
洛美沙星(NY - 198)是一种新型4 - 喹诺酮类化疗药物,作用于DNA回旋酶系统。与其他一些新型4 - 喹诺酮化合物一样,洛美沙星(LFLX)是具有潜在眼科应用价值的抗菌药物。本研究的主要目的是对LFLX的眼毒性进行初步研究。用四种浓度的LFLX(10、30、100和300微克/毫升)对色素兔角膜上皮细胞的第一代传代培养物进行测试。评估细胞数量、蛋白质含量、中性红染色和伤口愈合情况。结果表明,较低浓度(10和30微克/毫升)无影响,而最高浓度具有显著的细胞毒性作用。药代动力学数据显示,角膜和其他眼部结构中的峰值低于40微克/克(局部应用0.3%),另一方面,MIC值范围为小于或等于0.05至16微克/毫升。因此,根据我们的结果,这些“临界”浓度没有细胞毒性作用。由此得出结论,洛美沙星可能是一种用于局部眼科开发的有用药物。