Diamond J P, White L, Leeming J P, Bing Hoh H, Easty D L
University of Bristol, Department of Ophthalmology, Bristol Eye Hospital.
Br J Ophthalmol. 1995 Jun;79(6):606-9. doi: 10.1136/bjo.79.6.606.
This study was designed to assess the relative corneal penetration of topical drops of three antibiotics and to relate those levels to minimum inhibitory concentrations for organisms associated with bacterial keratitis.
Four drops of each of ciprofloxacin, norfloxacin, and ofloxacin (0.3% topical ophthalmic preparations) were given to 12 patients undergoing corneal transplantation. After the recipient tissue was removed, corneal drug penetration was measured using high performance liquid chromatography.
Intracorneal concentrations of ofloxacin (geometric mean 0.81 mg kg-1) were significantly higher than both ciprofloxacin (0.60 mg kg-1; p = 0.048) and norfloxacin (0.54 mg kg-1; p = 0.012). Ciprofloxacin and norfloxacin concentrations did not differ significantly (p = 0.33).
Review of the minimum inhibitory concentrations of the fluoroquinolones against ocular pathogens reveals that ciprofloxacin is more potent than ofloxacin against many bacteria; ofloxacin is in turn more potent than norfloxacin. These data favour the selection of ciprofloxacin and ofloxacin rather than norfloxacin for the empirical treatment of corneal infection. The greater potency of ciprofloxacin offsets the superior penetration of ofloxacin. There is a need for improved clinical trial data concerning the use of fluoroquinolone eyedrops in ulcerative keratitis; some encouraging data are available for ciprofloxacin but not (in humans) for norfloxacin or ofloxacin.
本研究旨在评估三种抗生素局部滴眼液的相对角膜穿透性，并将这些水平与细菌性角膜炎相关病原体的最低抑菌浓度相关联。
给12例接受角膜移植的患者分别滴入4滴环丙沙星、诺氟沙星和氧氟沙星（0.3%局部眼科制剂）。受体组织切除后，采用高效液相色谱法测量角膜药物穿透性。
氧氟沙星的角膜内浓度（几何均值0.81mg·kg⁻¹）显著高于环丙沙星（0.60mg·kg⁻¹；p = 0.048）和诺氟沙星（0.54mg·kg⁻¹；p = 0.012）。环丙沙星和诺氟沙星的浓度差异不显著（p = 0.33）。
回顾氟喹诺酮类药物对眼部病原体的最低抑菌浓度发现，环丙沙星对许多细菌的抗菌活性比氧氟沙星更强；氧氟沙星又比诺氟沙星更强。这些数据支持在角膜感染的经验性治疗中选择环丙沙星和氧氟沙星而非诺氟沙星。环丙沙星更强的抗菌活性抵消了氧氟沙星更好的穿透性。需要有关于氟喹诺酮类滴眼液在溃疡性角膜炎中应用的改进的临床试验数据；环丙沙星有一些令人鼓舞的数据，但诺氟沙星和氧氟沙星（在人类中）没有。
