Ocular Penetration and Pharmacokinetics of Topical Gatifloxacin 0.3% and Moxifloxacin 0.5% Ophthalmic Solutions After Keratoplasty.

Author(s): Holland EJ, Lane SS, Kim T, Raizman M, Dunn S

Affiliation(s): From the *Cincinnati Eye Institute, Edgewood, KY; the daggerAssociated Eye Care, Stillwater, MN; the double daggerDuke University Eye Center, Durham, NC; section signOphthalmic Consultants of Boston, Boston, MA; and paragraph signMichigan Cornea Consultants, Southfield, MI.

Publication date & source: 2008-04, Cornea., 27(3):314-319.

Publication type:

PURPOSE:: To compare the corneal and aqueous penetration and pharmacokinetics of gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions and their effect on corneal reepithelialization after penetrating keratoplasty. METHODS:: In this randomized, open-label, parallel-controlled study, corneal and aqueous penetration and the pharmacokinetic parameters of topically applied gatifloxacin 0.3% and moxifloxacin 0.5% (2 preoperative doses of 1 drop given 5 minutes apart) were estimated by using a sparse sampling method. Corneal and aqueous samples were collected 0.25, 0.5, 1, or 2 hours after the final dose. The concentration was determined by a high-performance liquid chromatography method. Stromal Cmax:MBC50 (maximum drug concentration in serum to 50% minimum bactericidal concentration) ratios for selected ocular pathogens were also assessed. Postoperative corneal reepithelialization at days 1, 3, and 7 was evaluated and compared between groups. RESULTS:: The calculated pharmacokinetic parameters were higher with moxifloxacin 0.5% than with gatifloxacin 0.3%. The stromal Cmax was 48.5 versus 15.7 mug/g (P = 0.04), and the stromal AUC0-2 (area under the concentration-time curve from 0 to 2 hours) was 30.9 versus 13.6 mug.h/g (P < 0.05). The endothelial Cmax was 76.1 versus 7.3 mug/g (P > 0.05), and the endothelial AUC0-2 was 43.9 versus 9.8 mug.h/g (P < 0.05). The aqueous Cmax was 0.9 versus 0.3 mug/mL (P > 0.05), and the aqueous AUC0-2 was 1.2 versus 0.4 mug.h/mL (P < 0.05). Stromal Cmax:MBC50 ratios were higher in the moxifloxacin 0.5% group for each pathogen tested. The corneal reepithelialization rates were comparable between groups. CONCLUSIONS:: Topical preoperative moxifloxacin 0.5% achieved greater corneal and aqueous penetration than did gatifloxacin 0.3%. The clinical significance of this difference is not known. Postoperative use of these agents had similar effects on corneal reepithelialization.