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在兔眼内炎模型中第二代、第三代和第四代局部用氟喹诺酮类药物向房水和玻璃体的渗透情况。

Penetration of second-, third-, and fourth-generation topical fluoroquinolone into aqueous and vitreous humour in a rabbit endophthalmitis model.

作者信息

Yağci R, Oflu Y, Dinçel A, Kaya E, Yağci S, Bayar B, Duman S, Bozkurt A

机构信息

Department of Ophthalmology, Ankara Training and Research Hospital, Ankara, Turkey.

出版信息

Eye (Lond). 2007 Jul;21(7):990-4. doi: 10.1038/sj.eye.6702414. Epub 2006 May 26.

DOI:10.1038/sj.eye.6702414
PMID:16732216
Abstract

AIMS

This study was designed to investigate the penetration of second-, third- and fourth-generation topical fluoroquinolone into aqueous and vitreous humour in a rabbit endophthalmitis model.

METHODS

Thirty New Zealand white rabbits were divided into six groups. Left eye was infected with an intravitreal inoculum of Staphylococcus aureus. Groups 1, 2, 3, 4, and 5 received topical ofloxacin, ciprofloxacin, lomefloxacin, levofloxacin, or moxifloxacin treatment 24 h after the inoculation, respectively. No treatment was given to group 6 as the control group (n=5). Aqueous and vitreous samples were obtained 30 min after the last drop. High-performance liquid chromatography was used to determine the fluoroquinolone concentration.

RESULTS

In the normal and inflamed eyes, mean aqueous concentrations of ofloxacin were 1.90 and 2.69 mug/ml, ciprofloxacin were 2.16 and 3.65 mug/ml, lomefloxacin were 3.54 and 1.19 mug/ml, levofloxacin were 2.89 and 9.41 mug/ml, and moxifloxacin were 4.92 and 43.33 mug/ml, respectively. Mean vitreous concentrations of ofloxacin were 0.25 and 0.07 mug/ml, ciprofloxacin were 0.08 and 0.32 mug/ml, lomefloxacin were 0.001 and 0.03 mug/ml, levofloxacin were 0.03 and 0.09 mug/ml, and moxifloxacin were 0.28 and 2.68 mug/ml, in normal and inflamed eyes, respectively. Moxifloxacin achieved a significantly higher concentration in aqueous and vitreous humour of infected eyes compared with ofloxacin (P<0.01), ciprofloxacin (P<0.05), lomefloxacin (P<0.01), and levofloxacin (P<0.05).

CONCLUSION

This study demonstrated that fourth-generation fluoroquinolone, moxifloxacin, seems to have better penetration to inflamed ocular tissues in rabbit.

摘要

目的

本研究旨在探讨在兔眼内炎模型中第二代、第三代和第四代局部用氟喹诺酮类药物在房水和玻璃体内的渗透情况。

方法

30只新西兰白兔分为6组。左眼经玻璃体内接种金黄色葡萄球菌感染。接种后24小时,第1、2、3、4和5组分别接受局部用氧氟沙星、环丙沙星、洛美沙星、左氧氟沙星或莫西沙星治疗。第6组不进行治疗作为对照组(n = 5)。在最后一滴用药30分钟后采集房水和玻璃体样本。采用高效液相色谱法测定氟喹诺酮类药物浓度。

结果

在正常眼和炎症眼中,氧氟沙星的平均房水浓度分别为1.90和2.69μg/ml,环丙沙星分别为2.16和3.65μg/ml,洛美沙星分别为3.54和1.19μg/ml,左氧氟沙星分别为2.89和9.41μg/ml,莫西沙星分别为4.92和43.33μg/ml。在正常眼和炎症眼中,氧氟沙星的平均玻璃体浓度分别为0.25和0.07μg/ml,环丙沙星分别为0.08和0.32μg/ml,洛美沙星分别为0.001和0.03μg/ml,左氧氟沙星分别为0.03和0.09μg/ml,莫西沙星分别为0.28和2.68μg/ml。与氧氟沙星(P < 0.01)、环丙沙星(P < 0.05)、洛美沙星(P < 0.01)和左氧氟沙星(P < 0.05)相比,莫西沙星在感染眼的房水和玻璃体内达到显著更高的浓度。

结论

本研究表明,第四代氟喹诺酮类药物莫西沙星在兔眼中似乎对炎症眼组织具有更好的渗透性。

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