去甲万古霉素兔眼眼内药代动力学研究

Intraocular Pharmacokinetics of Demethylvancomycin in Normal Rabbit Eyes

目的研究去甲万古霉素玻璃体注射和结膜下注射两种给药途径的兔眼眼内药代动力学,为临床治疗敏感菌引起的感染性眼病提供依据。方法健康成年白兔36只,随机分为玻璃体注射组和结膜下注射组,均注射1mg 去甲万古霉素。各组房水、玻璃体样品采用高效液相色谱法检测。结果玻璃体注射组在试验观察的48h 内玻璃体及房水中药物浓度均高于大多数革兰氏阳性菌的最低抑菌浓度(minimal inhibitoryconcentration MIC)。结膜下注射组在试验72h 内玻璃体中药物浓度低于 MIC,房水中可达有效浓度。结论玻璃体注射1mg 去甲万古霉素可用于治疗感染性眼内炎,结膜下注射仅对眼前段感染有效,在眼后段不能达到治疗水平。(中国眼耳鼻喉科杂志,2005,5:347～349)

Purpose To investigate the intraocular pharmaeokinetics of intravitreal and subconjunetival demethylvaneomyein in normal rabbit eyes.Methods Thirty-six New Zealand rabbits （72 eyes） were divided into two groups of 18 animals （36 eyes） each. Demethylvancomycin of lmg was injected into mid-vitreous cavity of one group and subeonjunetival injection was performed with the same dose in another group. The demethylvancomycin concentration in the samples was determined by high-performance liquid chromatography （HPLC）. Results In the intravitreal injection group, the therapeutic drug concentration was present in the vitreous and aqueous 48 hours post-injection in all eyes. In subconjunetival injection group, the drug concentrations in vitreous body were lower than minimal inhibitory concentration （MIC） of the most gram-positive bacteria. The therapeutic drug concentration could be reached and last for 72 hours in aqueous. Conclusion The intravitreal injection of ling demethylvancomycin could be used in endophthalmitis induced by sensitive bacteria. Subconjunctival injection of same dosage was applied in infectious ocular disease of anterior segment.