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K Yamada, M Yamada, H Mochizuki, M Kawai, Y Mashima; Aqueous Humor Levels of Topically Applied Levofloxacin, Norfloxacin, and Lomefloxacin in the Same Human Eyes . Invest. Ophthalmol. Vis. Sci. 2002;43(13):1577.
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Purpose: This study was designed to assess the relative penetration of topical eyedrops of three fluoroquinolones, levofloxacin, norfloxacin, and lomefloxacin, into the aqueous humor of humans. Methods: Fifty-nine cataract patients (36 females, 23 males) received three drops of each of 0.5% levofloxacin, 0.3% norfloxacin, and 0.3% lomefloxacin at 15 min intervals, beginning 90 minutes before surgery. At the beginning of the cataract surgery, 50 µL of aqueous humor was aspirated from the anterior chamber and stored at -80 ° C until analysis. The samples were analyzed for drug concentration using high-performance liquid chromatography. The elution was performed using ODS-80 column with a mobile phase of 85:15 mixture of pH 3.0, 0.05M phosphoric acid and acetonitrile. Flow rate was set at 0.7 mL/min and detection was by fluorescence (excitation 290 nm, emission 470 nm). The detection limit of the analysis was 0.05 mg/mL for each drug. Results: Five patients were excluded because sample volume was insufficient. Norfloxacin was detected only in 3 patients. A mean aqueous humor level of norfloxacin was 0.10 ± 0.02 µg/mL (mean ± standard deviation, n = 3). Levofloxacin was detected in all cases with a mean aqueous humor level of 0.60 ± 0.28 µg/mL (n = 54). Lomefloxacin was not detected in 10 patients. A mean aqueous humor level of lomefloxacin was 0.23 ± 0.11 µg/mL (n = 44). Conclusions: The mean concentration of levofloxacin in the aqueous humor was higher than those of norfloxacin and lomefloxacin. These data favour the selection of levofloxacin rather than norfloxacin and lomefloxacin for the prophylaxis of postoperative infections.
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