Coco R M, López M I, Pastor J C, Nozal M J
Ocular Pharmacology Unit, Instituto de Oftalmobiología Aplicada, University of Valladolid, Spain.
J Ocul Pharmacol Ther. 1998 Dec;14(6):555-63. doi: 10.1089/jop.1998.14.555.
The purpose of this study was to determine the pharmacokinetics governing the distribution and elimination of intravitreally injected vancomycin in normal and infected rabbit eyes. Two groups each of 36 pigmented animals were used. Group 1 served as control. In Group 2, experimental endophthalmitis was induced in the right vitreous by inoculation with Staphylococcus aureus. Once endophthalmitis developed, a vancomycin solution was injected. Four animals from each group were killed at nine time points post-injection, the vitreous and aqueous were removed, and blood samples were taken for HPLC analysis. Data analysis was performed using the RSTRIP program. The half-lives were 69 hours in normal vitreous and 14.53 hours in infected vitreous. Therapeutic drug levels were present in the vitreous 84 hours post-injection in all eyes; they were detected from 2 to 48 hours in normal aqueous but at lower levels in the infected ones. Kv and Ca/Cv ratios suggested that the primary route of elimination was across the retina and the anterior chamber in normal eyes, and via the retina in infected eyes. Results indicate that pharmacokinetic parameters change in pathological conditions, which may help establish better treatment guidelines for endophthalmitis.
本研究的目的是确定玻璃体内注射万古霉素在正常和感染兔眼中分布与消除的药代动力学。使用了两组，每组36只有色动物。第1组作为对照。在第2组中，通过接种金黄色葡萄球菌在右眼玻璃体内诱发实验性眼内炎。一旦眼内炎形成，即注射万古霉素溶液。注射后在9个时间点处死每组4只动物，取出玻璃体和房水，并采集血样进行高效液相色谱分析。使用RSTRIP程序进行数据分析。正常玻璃体中的半衰期为69小时，感染玻璃体中的半衰期为14.53小时。所有眼在注射后84小时玻璃体中均存在治疗药物水平；在正常房水中2至48小时可检测到治疗药物水平，但在感染房水中水平较低。Kv和Ca/Cv比值表明，正常眼中主要的消除途径是穿过视网膜和前房，而感染眼中是通过视网膜。结果表明，病理状态下药代动力学参数会发生变化，这可能有助于制定更好的眼内炎治疗指南。
