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J. Yoshida, A. Kim, K. A. Pratzer, W. J. Stark; Aqueous Penetration of Moxifloxacin 0.5% Ophthalmic Solution and Besifloxacin 0.6% Ophthalmic Suspension in Cataract Surgery Patients. Invest. Ophthalmol. Vis. Sci. 2010;51(13):5718.
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To determine the aqueous humor concentrations of commercially available moxifloxacin 0.5% ophthalmic solution and besifloxacin 0.6% ophthalmic suspension following routine preoperative topical dosing in patients undergoing cataract surgery.
A prospective, randomized, parallel, double-masked clinical trial was performed. Subjects were given one drop of moxifloxacin 0.5% ophthalmic solution (n = 23) or besifloxacin 0.6% ophthalmic suspension (n = 25) which was administered every 10 minutes for a total of 4 doses beginning 1 hour prior to routine cataract surgery. Aqueous humor was sampled via paracentesis and antibiotic concentrations were determined using validated high performance liquid chromatography (HPLC) procedures.
The aqueous concentration of antibiotic was detectable in 100% (23/23) of the subjects who received moxifloxacin compared to 40% (10/25) of the subjects who received besifloxacin (p < 0.0001, Pearson’ chi-square test). The mean aqueous drug concentration for moxifloxacin (1.6108µg/ml) was 50-fold higher (p < 0.0001, Wilcoxon test) than for besifloxacin (0.0319µg/ml). When comparing the subset of aqueous samples with detectable levels of antibiotic, the mean moxifloxacin concentration (1.6108µg/ml) was 38-fold higher (p < 0.0001) than that of besifloxacin (0.0422µg/ml).
After preoperative topical administration, moxifloxacin 0.5% ophthalmic solution achieved a 50-fold higher concentration in aqueous humor compared with besifloxacin 0.6% ophthalmic suspension. Besifloxacin was undetectable in more than half of the aqueous humor samples.
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