Alfaro D V, Pince K, Park J, Runyan T, Ryan S J, Liggett P E
Department of Ophthalmology, University of Southern California School of Medicine, Doheny Eye Institute, Los Angeles.
Retina. 1992;12(3 Suppl):S3-6. doi: 10.1097/00006982-199212031-00002.
Intraocular concentrations of systemically administered gentamicin and cefazolin in eyes after a standard penetrating ocular injury were measured to determine the effect of eye injury on ocular pharmacokinetics. Twenty pigmented rabbits were divided into two groups. A standard, 8-mm wound was made at the pars plana of one eye in each animal. Group 1 consisted of 10 rabbits that were treated with cefazolin (75 mg/kg), and Group 2 consisted of 10 rabbits that were given gentamicin (2 mg/kg). Fellow eyes, which sustained no trauma, served as control eyes. All groups received intravenous injections every 8 hours for 72 hours, beginning immediately after repair of the wound. After 72 hours, samples were obtained from the anterior chamber, vitreous cavity, and serum. Standardized bioassays for detection of gentamicin or cefazolin were performed. Significant concentrations of intravitreal cefazolin (9.6 micrograms/ml) and gentamicin (0.60 micrograms/ml) were found in the traumatized eyes in comparison to control eyes (P = 0.0001; P = 0.006). Cefazolin exhibited excellent penetration, achieving concentrations well above minimum inhibitory concentration values for most organisms. Gentamicin levels, however, were well below acceptable therapeutic levels. This study suggests that systemically administered cefazolin can achieve significant intravitreal penetration at minimum inhibitory concentrations after penetrating injury.
为了确定眼外伤对眼药代动力学的影响，我们测量了标准穿透性眼外伤后全身给药的庆大霉素和头孢唑林在眼内的浓度。将20只有色家兔分为两组。在每只动物的一只眼的睫状体平坦部制作一个标准的8毫米伤口。第1组由10只接受头孢唑林（75毫克/千克）治疗的家兔组成，第2组由10只给予庆大霉素（2毫克/千克）的家兔组成。未受创伤的对侧眼作为对照眼。所有组在伤口修复后立即开始，每8小时静脉注射一次，共72小时。72小时后，从前房、玻璃体腔和血清中获取样本。进行了检测庆大霉素或头孢唑林的标准化生物测定。与对照眼相比，在受伤眼中发现玻璃体内头孢唑林（9.6微克/毫升）和庆大霉素（0.60微克/毫升）的浓度显著升高（P = 0.0001；P = 0.006）。头孢唑林表现出优异的穿透力，其浓度远高于大多数微生物的最低抑菌浓度值。然而，庆大霉素水平远低于可接受的治疗水平。这项研究表明，全身给药的头孢唑林在穿透性损伤后能够在最低抑菌浓度下实现显著的玻璃体内穿透。
