Koul S, Philipson A, Philipson B T, Arvidson S
Department of Ophthalmology, Karolinska Hospital, Stockholm, Sweden.
Eur J Ophthalmol. 1993 Apr-Jun;3(2):61-5. doi: 10.1177/112067219300300202.
The pharmacokinetics of cefuroxime was studied in the inflamed rabbit eye employing subconjunctival, intravitreal and combined intravitreal-intravenous routes of administration to study the intraocular levels and the duration of minimum inhibitory concentrations (MIC) of the antibiotic in the vitreous and in the aqueous. A standard inoculum of viable S. aureus was injected into the vitreous of 36 pigmented rabbits to establish experimental endophthalmitis. A biological method was used for the antibiotic assay. Penetration of systemically and subconjunctivally administered-cefuroxime into the inflamed vitreous was poor. Intraocular inflammation increased the clearance of the intravitreally injected cefuroxime. A dose of 75 mg subconjunctivally produced levels in the aqueous far exceeding MIC for over six hours. Penetration of intravitreally injected cefuroxime into the aqueous was poor, inconsistent and short lasting. Following a single intravitreal injection of 1000 micrograms cefuroxime, levels exceeding the MIC for common ocular pathogens persisted in the vitreous for at least 24 hours but supplementation with intravenous cefuroxime neither increased the intraocular levels nor delayed the clearance of the intravitreally injected antibiotic.
采用结膜下、玻璃体内及玻璃体内-静脉联合给药途径，在兔眼炎症模型中研究头孢呋辛的药代动力学，以探讨抗生素在玻璃体和房水中的眼内浓度及最低抑菌浓度（MIC）持续时间。将标准接种量的活金黄色葡萄球菌注入36只有色兔的玻璃体中，以建立实验性眼内炎。采用生物学方法进行抗生素检测。全身给药和结膜下给药的头孢呋辛进入炎症玻璃体的穿透性较差。眼内炎症增加了玻璃体内注射头孢呋辛的清除率。结膜下注射75mg剂量可使房水中的药物浓度超过MIC达6小时以上。玻璃体内注射头孢呋辛进入房水的穿透性较差、不稳定且持续时间短。单次玻璃体内注射1000μg头孢呋辛后，玻璃体中超过常见眼部病原体MIC的浓度至少持续24小时，但静脉补充头孢呋辛既未增加眼内药物浓度，也未延迟玻璃体内注射抗生素的清除。
