Gatti G, Panozzo G
School of Pharmacy, University of California, San Francisco, USA.
Antimicrob Agents Chemother. 1995 Feb;39(2):549-52. doi: 10.1128/AAC.39.2.549.
The effect of inflammation on the intraocular penetration of ofloxacin was studied in 20 albino rabbits (New Zealand White). Inflammation was induced in the left eye by inoculation of a suspension of 10(9) CFU of heat-killed Staphyloccus epidermidis per 0.1 ml of saline solution (0.9%) in the midvitreous cavity. The other eye was kept as a control. Twenty-four hours following inoculation, ofloxacin was administered in the marginal ear vein at a dose of 15 mg/kg over 20 min with an infusion pump. Animals were sacrificed at different times up to 24 h following drug administration. Ofloxacin levels were determined in aqueous humor, vitreous humor, and serum by a bioassay. Inflammation was scored on the basis of perilimbal and corneal reactions and vitreoretinal statuses. Inflammation had a relevant effect on intraocular penetration of ofloxacin, with levels in the ocular fluids of the inflamed eye markedly exceeding the ones of the control eye. In the uninflamed eye, the levels were rapidly decaying below assay sensitivity and were no longer detectable at approximately 5 h following drug administration while they were still detectable in both ocular fluids of the inflamed eye at 24 h. Ofloxacin levels in the ocular fluids of the inflamed eye were superior to the MIC for several of the bacteria which commonly cause endophthalmitis, including Staphylococcus epidermidis, Staphylococcus aureus, most members of the family Enterobacteriaceae, Haemophilus influenzae, and strains of Pseudomonas aeruginosa.
在20只白化兔(新西兰白兔)中研究了炎症对氧氟沙星眼内渗透的影响。通过向左眼玻璃体内腔注射每0.1毫升生理盐水(0.9%)含10⁹CFU热灭活表皮葡萄球菌的悬液诱导炎症。另一只眼作为对照。接种后24小时,用输液泵经耳缘静脉以15毫克/千克的剂量在20分钟内给予氧氟沙星。给药后在长达24小时的不同时间处死动物。通过生物测定法测定房水、玻璃体和血清中的氧氟沙星水平。根据角膜缘和角膜反应以及玻璃体视网膜状态对炎症进行评分。炎症对氧氟沙星的眼内渗透有显著影响,炎症眼眼内液中的水平明显超过对照眼。在未发炎的眼中,给药后约5小时,水平迅速降至检测灵敏度以下且不再可检测到,而在炎症眼的两种眼内液中在24小时时仍可检测到。炎症眼眼内液中的氧氟沙星水平高于几种常见引起眼内炎的细菌的最低抑菌浓度,包括表皮葡萄球菌、金黄色葡萄球菌、肠杆菌科的大多数成员、流感嗜血杆菌和铜绿假单胞菌菌株。