Hariprasad Seenu M, Mieler William E, Shah Gaurav K, Blinder Kevin J, Apte Rajendra S, Holekamp Nancy M, Thomas Matthew A, Chi Jingduan, Prince Randall A
Barnes Retina Institute, Department of Ophthalmology and Visual Science, Washington University School of Medicine, St Louis, Missouri, USA.
Trans Am Ophthalmol Soc. 2004;102:149-55; discussion 155-7.
To determine penetration of moxifloxacin 0.5% into human aqueous and vitreous via topical and collagen shield routes of administration.
Moxifloxacin 0.5% was administered prior to vitrectomy surgery through one of three routes: topical drops every 2 hours for 3 days, versus topical drops every 6 hours for 3 days, versus delivery using a 24-hour dissolvable cross-linked corneal collagen shield. Aqueous and vitreous moxifloxacin concentrations were assayed using high-performance liquid chromatography.
Mean moxifloxacin concentrations in the every-2-hour group for aqueous (n = 9) and vitreous (n = 10) were 2.28 +/- 1.23 microg/mL and 0.11 +/- 0.05 microg/mL, respectively. Mean moxifloxacin concentrations in the every-6-hour group for aqueous (n = 10) and vitreous (n = 9) were 0.88 +/- 0.88 microg/mL and 0.06 +/- 0.06 microg/mL, respectively. Levels of minimum inhibitory concentration at which 90% of isolates are inhibited (MIC90) were far exceeded in the aqueous for a wide spectrum of pathogens that most commonly cause postoperative endophthalmitis. Moxifloxacin concentration in the vitreous did not exceed the MIC90 for several key organisms. Delivery of moxifloxacin via a collagen shield revealed a mean aqueous concentration of 0.30 +/- 0.17 microg/mL 4 hours after placement (n = 5). Vitreous levels at 4 hours, as well as aqueous and vitreous levels at 24 hours, were negligible using this route of administration.
The findings of this investigation reveal that topically administered moxifloxacin 0.5% can achieve relatively high aqueous concentrations. Although aqueous moxifloxacin levels achieved through the use of a collagen shield delivery device are lower, there are several advantages to this route of delivery that make it appealing in the immediate postoperative period. Future studies will be needed to precisely define the role of fourth-generation fluoroquinolones and presoaked collagen shields in the prophylaxis or management of intraocular infections.
通过局部给药和胶原盾给药途径，测定0.5%莫西沙星在人房水和玻璃体中的渗透情况。
在玻璃体切除术前，通过三种途径之一给予0.5%莫西沙星：每2小时局部滴眼，共3天；或每6小时局部滴眼，共3天；或使用24小时可溶解的交联角膜胶原盾给药。采用高效液相色谱法测定房水和玻璃体中莫西沙星的浓度。
每2小时滴眼组房水（n = 9）和玻璃体（n = 10）中莫西沙星的平均浓度分别为2.28±1.23μg/mL和0.11±0.05μg/mL。每6小时滴眼组房水（n = 10）和玻璃体（n = 9）中莫西沙星的平均浓度分别为0.88±0.88μg/mL和0.06±0.06μg/mL。对于大多数常见的引起术后眼内炎的病原体，房水中莫西沙星的浓度远远超过90%分离株被抑制时的最低抑菌浓度（MIC90）。玻璃体中莫西沙星的浓度未超过几种关键病原体的MIC90。通过胶原盾给药的莫西沙星，放置4小时后房水的平均浓度为0.30±0.17μg/mL（n = 5）。采用该给药途径，4小时时玻璃体中的药物浓度以及24小时时房水和玻璃体中的药物浓度均可忽略不计。
本研究结果表明，局部应用0.5%莫西沙星可达到相对较高的房水浓度。虽然通过胶原盾给药装置获得的房水莫西沙星浓度较低，但该给药途径有几个优点，使其在术后即刻具有吸引力。未来需要进一步研究来精确确定第四代氟喹诺酮类药物和预浸胶原盾在预防或治疗眼内感染中的作用。
