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S.M. Robertson, M. Sanders, D. Jasheway, D. Trawick, J. Veltman, S. Hamner, B.A. Schlech, R. Hilaski, D.C. Dahlin; Penetration and Distribution of Moxifloxacin and Ofloxacin into Ocular Tissues and Plasma Following Topical Ocular Administration to Pigmented Rabbits . Invest. Ophthalmol. Vis. Sci. 2003;44(13):1454.
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Purpose: To measure the ocular penetration and distribution of moxifloxacin and ofloxacin into cornea, aqueous humor, iris-ciliary body, tear film and plasma following a single topical ocular administration of 0.3% solutions to rabbits. Methods: The eyes of male Dutch belted rabbits were dosed with a single drop (30 µL) of either 0.3% moxifloxacin solution or ofloxacin 0.3% (OCUFLOX®). Aqueous humor, cornea, iris-ciliary body, tear film and plasma were collected up to 48 hours for analyses of drug concentrations by reverse phase HPLC. Results: Moxifloxacin was well absorbed into the eye and achieved relatively high concentrations in ocular tissues 30 minutes after the single dose (µg/g: cornea: 12.5; aqueous humor: 1.8; iris-ciliary body: 6.3; tear film 10.3). Maximal concentrations of moxifloxacin were typically 2-fold higher than those found for ofloxacin and remained 2-fold higher over the course of the study. Even 48 hours after the single-drop instillation, moxifloxacin mean concentration in the cornea was 0.25 µg/g, which is about 4-fold above its MIC of 0.06 µg/mL for methicillin-susceptible Staphylococcus aureus. Conversely, ofloxacin cornea concentrations fell below the MIC for this organism of 0.5 µg/mL by 8 hours after dosing. The mean tear film concentration of moxifloxacin was 366 µg/mL at the initial 10-minute sampling time and remained at or above 1 µg/mL over 6 hours post-dose. Prolonged retention of moxifloxacin and ofloxacin was observed in the pigmented iris-ciliary body due to melanin binding which is characteristic of fluoroquinolones. Maximum plasma concentrations were about 0.01 µg/mL for both compounds and declined rapidly. Conclusions: These pharmacokinetic findings predict that significant antimicrobial levels of moxifloxacin can be achieved in ocular tissues after ocular instillation of a single drop or more of moxifloxacin solution at or above 0.3%. Moxifloxacin exhibited better penetration than ofloxacin into ocular tissues with no significant systemic exposure.
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