Oztürk F, Kortunay S, Kurt E, Inan U U, Ilker S S, Basci N, Bozkurt A
Celal Bayar University, Faculty of Medicine, Department of Ophthalmology, Manisa, Turkey.
Curr Eye Res. 1999 Dec;19(6):461-4. doi: 10.1076/ceyr.19.6.461.5277.
To study the penetration of ofloxacin into the aqueous and vitreous humors after long-term topical administration and to investigate the effects of inflammation on drug penetration in rabbits.
A standardized model of intraocular infection after penetrating injury was achieved in the right eyes of 16 rabbits. The animals were randomly and equally divided into two groups. The intact left eyes of the groups were maintained as the control. Ofloxacin eyedrops (0.3%) were instilled into all eyes at a frequency of 2 drops every hour for 7 hours in the first group and for 14 hours in the second group. Half an hour after the last drop, samples of the aqueous and vitreous humors were taken and ofloxacin concentrations were measured by using HPLC.
The mean aqueous humor concentrations of ofloxacin in control eyes after 7 and 14 hours of instillation were: 1.45 +/- 0.93 microg/ml and 2.48 +/- 0.33 microg/ml, respectively; those in infected eyes 2.35 +/- 1. 84 microg/ml and 3.49 +/- 1.47 microg/ml, respectively. However the differences among the groups were not significant (p > 0.05). The vitreous ofloxacin concentrations in the control eyes were similar after 7 and 14 hours of instillation (0.23 +/- 0.14 microg/ml, 0.27 +/- 0.10 microg/ml, respectively). In infected eyes, the mean vitreous ofloxacin concentration after 14 hour of instillation was significantly higher than that in control eyes (p < 0.05; 0.4 +/- 0. 09 microg/ml, 0.29 +/- 0.11 microg/ml, respectively). The mean vitreous ofloxacin concentration in infected eyes after 14 hours instillation was not significantly higher than that after 7 hours instillation.
Topical ofloxacin instillation for 7 or 14 hours yields aqueous concentrations above the MIC(90) for common ocular pathogens. Prolonged application and the presence of inflammation increased the penetration of ofloxacin into the vitreous humor.
研究长期局部应用氧氟沙星后其在房水和玻璃体内的渗透情况，并探讨炎症对兔眼药物渗透的影响。
在16只兔的右眼建立穿透伤后眼内感染的标准化模型。动物被随机等分为两组。两组动物完好的左眼作为对照。第一组每小时滴入2滴0.3%氧氟沙星滴眼液，共7小时；第二组共滴入14小时。最后一滴后半小时，采集房水和玻璃体样本，用高效液相色谱法测定氧氟沙星浓度。
滴入7小时和14小时后，对照眼房水中氧氟沙星的平均浓度分别为：1.45±0.93微克/毫升和2.48±0.33微克/毫升；感染眼分别为2.35±1.84微克/毫升和3.49±1.47微克/毫升。然而，两组间差异无统计学意义（p>0.05）。滴入7小时和14小时后，对照眼玻璃体内氧氟沙星浓度相似（分别为0.23±0.14微克/毫升、0.27±0.10微克/毫升）。在感染眼，滴入14小时后玻璃体内氧氟沙星平均浓度显著高于对照眼（p<0.05；分别为0.4±0.09微克/毫升、0.29±0.11微克/毫升）。感染眼滴入14小时后玻璃体内氧氟沙星平均浓度并不显著高于滴入7小时后。
局部滴入氧氟沙星7或14小时可使房水浓度高于常见眼部病原体的MIC(90)。延长用药时间和炎症的存在增加了氧氟沙星向玻璃体内的渗透。
