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M. B. McDonald, P. Bezwada; Penetration and Persistence of Levofloxacin, Moxifloxacin, and Gatifloxacin in Aqueous Humor. Invest. Ophthalmol. Vis. Sci. 2008;49(13):1987.
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© ARVO (1962-2015); The Authors (2016-present)
To compare fluoroquinolone concentrations over time in rabbit aqueous following administration of commercial formulation of 1.5% levofloxacin (LEV; Iquix®), 0.5% moxifloxacin (MOX; Vigamox®), or 0.3% gatifloxacin (GAT; Zymar®).
Rabbits were randomized to receive a single drop bilaterally of commercial ophthalmic fluoroquinolone formulations: 1.5% LEV (N=21), 0.5% MOX (N=21), or 0.3% GAT (N=21). Three animals in each group were sacrificed at 10 or 30 minutes or at 1, 2, 4, 8, or 12 hours post-dosing. Aqueous humor samples (n=6 per time point) were collected and analyzed using a validated method. Mean tissue concentrations were calculated for each time point. Drug exposure measured as area under the curve (AUC) from time of dosing was calculated by the linear trapezoid method.
MOX concentrations were greater than those of LEV or GAT during the first hour but declined more rapidly and were below detectable limits by 8 hrs. After 1 hr, LEV concentrations were higher than those of MOX and GAT. At 12 hrs post-instillation, only LEV concentrations were quantifiable. Drug exposure (AUC) to LEV was nearly three times that of GAT and 35% higher than MOX.
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