Kim Dianne H, Stark Walter J, O'Brien Terrence P, Dick James D
Anterior Segment and Cataract/Refractive Service, The Wilmer Eye Institute, Johns Hopkins University School of Medicine, Baltimore, Maryland 21287-9238, USA.
Ophthalmology. 2005 Nov;112(11):1992-6. doi: 10.1016/j.ophtha.2005.06.017. Epub 2005 Sep 23.
To measure the achievable perioperative aqueous concentration of the commercially available topically administered fourth generation fluoroquinolones, moxifloxacin 0.5% ophthalmic solution, and gatifloxacin 0.3% ophthalmic solution, and to correlate this concentration with the agents' biological efficacy in the aqueous humor of patients undergoing routine cataract surgery.
Prospective, randomized, parallel, double-masked, clinical trial.
Fifty patients undergoing cataract extraction.
Patients (n = 25) were given perioperative topical moxifloxacin 0.5% or topical gatifloxacin 0.3% (n = 25). One drop of antibiotic was administered every 10 minutes for 4 doses beginning 1 hour prior to surgery. Aqueous humor was sampled via paracentesis and antibiotic concentrations were determined using validated high performance liquid chromatography (HPLC) procedures. Dilution analyses were performed to determine the biological efficacy of the agents in the aqueous against Staphylococcus epidermidis, the most common cause of postcataract endophthalmitis.
Aqueous humor antibiotic concentrations were measured using HPLC and microdilution bioassay techniques. Biological activity was measured as minimal inhibitory dilution and minimal bactericidal dilution.
Aqueous humor concentrations for moxifloxacin via HPLC analysis were 1.80 (+/-1.21) microg/ml, whereas those for gatifloxacin were 0.48 (+/-0.34) microg/ml. This 3.8-fold difference in aqueous humor antibiotic concentrations was statistically significant (P = 0.00003). Similarly, the biological dilution analysis of the aqueous humor samples showed that moxifloxacin attained an estimated activity of 2.1 microg/ml, whereas the gatifloxacin activity was approximately 0.4 mug/ml, which represented a 4.9-fold difference.
This study demonstrated that after topically administered perioperative antibiotics with cataract surgery, moxifloxacin 0.5% ophthalmic solution achieved a statistically significantly higher concentration in aqueous humor compared with gatifloxacin (P = 0.00003). Results from the broth dilution analysis showed that moxifloxacin 0.5% was biologically more active against S. epidermidis than gatifloxacin 0.3% in aqueous humor after topical application. There were no adverse events reported, and incision wounds healed quickly and as expected.
测量市售局部给药的第四代氟喹诺酮类药物（0.5%莫西沙星滴眼液和0.3%加替沙星滴眼液）在围手术期所能达到的房水浓度，并将该浓度与这些药物在接受常规白内障手术患者房水中的生物学疗效相关联。
前瞻性、随机、平行、双盲临床试验。
50例接受白内障摘除术的患者。
患者（n = 25）在围手术期接受局部应用0.5%莫西沙星或局部应用0.3%加替沙星（n = 25）。从手术前1小时开始，每10分钟滴注一滴抗生素，共4剂。通过前房穿刺采集房水样本，并使用经过验证的高效液相色谱（HPLC）程序测定抗生素浓度。进行稀释分析以确定这些药物在房水中对白内障术后眼内炎最常见病因表皮葡萄球菌的生物学疗效。
使用HPLC和微量稀释生物测定技术测量房水抗生素浓度。生物学活性以最小抑菌稀释度和最小杀菌稀释度来衡量。
通过HPLC分析，莫西沙星的房水浓度为1.80（±1.21）μg/ml，而加替沙星的房水浓度为0.48（±0.34）μg/ml。房水抗生素浓度的这3.8倍差异具有统计学意义（P = 0.00003）。同样，房水样本的生物学稀释分析表明，莫西沙星的估计活性为2.1μg/ml，而加替沙星的活性约为0.4μg/ml，相差4.9倍。
本研究表明，在白内障手术围手术期局部应用抗生素后，0.5%莫西沙星滴眼液在房水中达到的浓度与加替沙星相比具有统计学显著差异（P = 0.00003）。肉汤稀释分析结果表明，局部应用后，0.5%莫西沙星在房水中对表皮葡萄球菌的生物学活性高于0.3%加替沙星。未报告不良事件，切口愈合迅速且符合预期。
