局部和口服氧氟沙星在炎症兔眼房水和玻璃体液中的渗透情况。

Penetration of topical and oral ofloxacin into the aqueous and vitreous humor of inflamed rabbit eyes.

作者信息

Oztürk F, Kurt E, Inan U U, Kortunay M C, Ilker S S, Başci N E, Bozkurt A

机构信息

Department of Ophthalmology. Faculy of Medicine, Kocatepe University, Afyon, Turkey.

出版信息

Int J Pharm. 2000 Aug 25;204(1-2):91-5. doi: 10.1016/s0378-5173(00)00482-8.

DOI:10.1016/s0378-5173(00)00482-8

PMID:11011990

Abstract

PURPOSE

This study aimed to investigate the penetration of topical and oral ofloxacin into aqueous humor and vitreous humor in post-traumatic endophthalmitis model in rabbits.

METHODS

A standardized intraocular infection after penetrating injury was made in the right eyes of 16 rabbits. Intraocular infection was induced by intravitreal injection of a suspension of Staphylococcus aureus. The intact left eyes were maintained as controls. The animals were divided randomly into two groups. (1) In the topical group, two drops of ofloxacin 0.3% eyedrops were instilled to both eyes every 30 min for 4 h. (2) In the topical-oral group, two doses of 25 mg/kg of ofloxacin at 12-h intervals were given orally, then the protocol of the first group was applied. Aqueous and vitreous humor samples were taken 30 min after the last drop. Ofloxacin concentrations were measured by using HPLC.

RESULTS

Mean aqueous levels of ofloxacin in control eyes were: 3.25 +/- 2.55 microg/ml in topical group. 4.58 +/- 5.39 microg/ml in topical-oral group. Mean aqueous levels in inflamed eyes were: 5.21 +/- 4.55 microg/ml in topical group, 10.34 +/- 8.88 microg/ml in topical-oral group. Mean vitreous levels of ofloxacin in control eyes were: 0.17 +/- 0.07 microg/ml in topical group, 1.30 +/- 1.23 microg/ml in topical-oral group. Mean vitreous levels in inflamed eyes were: 0.35 +/- 0.22 microg/ml in topical group, 3.48 +/- 2.69 microg/ml in topical-oral group. There was no significant difference among the groups (P > 0.05), however.

CONCLUSIONS

The result of this study suggests that oral supplementation of ofloxacin to topical instillation increased the ocular levels of ofloxacin in the post-traumatic endophthalmitis model. Mean drug concentrations in aqueous and vitreous humors were above the 90% minimum inhibitory concentrations (MIC90) for most of the common microorganisms causing endophthalmitis in all eyes, except in the vitreous humors of the intact eyes instilled topically.

摘要

目的

本研究旨在探讨在兔眼外伤性眼内炎模型中局部和口服氧氟沙星在房水和玻璃体液中的渗透情况。

方法

对16只兔的右眼进行标准化的穿透伤后眼内感染。通过玻璃体内注射金黄色葡萄球菌悬液诱导眼内感染。完整的左眼作为对照。将动物随机分为两组。（1）局部用药组，每30分钟给双眼滴注两滴0.3%氧氟沙星滴眼液，共4小时。（2）局部 - 口服组，每12小时口服两剂25mg/kg氧氟沙星，然后采用第一组的用药方案。在最后一滴用药后30分钟采集房水和玻璃体液样本。使用高效液相色谱法测量氧氟沙星浓度。

结果

对照组眼中氧氟沙星的平均房水浓度为：局部用药组为3.25±2.55μg/ml，局部 - 口服组为4.58±5.39μg/ml。炎症眼中氧氟沙星的平均房水浓度为：局部用药组为5.21±4.55μg/ml，局部 - 口服组为10.34±8.88μg/ml。对照组眼中氧氟沙星的平均玻璃体液浓度为：局部用药组为0.17±0.07μg/ml，局部 - 口服组为1.30±1.23μg/ml。炎症眼中氧氟沙星的平均玻璃体液浓度为：局部用药组为0.35±0.22μg/ml，局部 - 口服组为3.48±2.69μg/ml。然而，各组之间无显著差异（P>0.05）。