Concentrations of besifloxacin, gatifloxacin, and moxifloxacin in human conjunctiva after topical ocular administration

• Published in: Clinical ophthalmology (Auckland, N.Z.) Vol. 4; no. default; pp. 331 - 341
• Main Authors: Torkildsen, Gail, Proksch, Joel W, Shapiro, Aron, Lynch, Stephanie K, Comstock, Timothy L
• Format: Journal Article
• Language: English
• Published: New Zealand Taylor & Francis Ltd 01.01.2010; Dove Press; Dove Medical Press
• Subjects: Antibiotics; besifloxacin; conjunctivitis; fluoroquinolone; minimum inhibitory concentration; Ophthalmology; Original Research; pharmacokinetics; pharmacokinetics; besifloxacin; conjunctivitis; fluoroquinolone; minimum inhibitory concentration
• ISSN: 1177-5483; 1177-5467; 1177-5483
• DOI: 10.2147/OPTH.S9163

To evaluate the pharmacokinetic properties of besifloxacin, gatifloxacin, and moxifloxacin in the conjunctival tissue of healthy volunteers after topical application. One-hundred eight (108) subjects were randomly assigned to receive one drop of besifloxacin (0.6% suspension), gatifloxacin (0.3% solution), or moxifloxacin (0.5% solution) ophthalmic formulations in one eye prior to conjunctival biopsy. Conjunctival samples were taken from subjects at either 15 minutes, 30 minutes, 2 hours, 6 hours, 12 hours, or 24 hours after dosing. All three fluoroquinolones reached a peak mean concentration 15 minutes after dosing. The mean concentrations of besifloxacin, gatifloxacin, and moxifloxacin at 15 minutes were 2.30 +/- 1.42 mug/g, 4.03 +/- 3.84 mug/g, and 10.7 +/- 5.89 mug/g, respectively. Concentrations decreased with each subsequent time point. At 24 hours after dosing, concentrations of besifloxacin were measurable in 4 of 6 subjects, compared with 3 of 6 subjects for gatifloxacin and 2 of 6 subjects for moxifloxacin. Besifloxacin had the greatest mean residence time (4.7 hours) in the conjunctival tissue. With regard to methicillin-resistant strains of Staphylococcus aureus and Staphylococcus epidermidis, besifloxacin had the greatest area-under-the-curve (AUC) to MIC(90) ratio. Nine percent (9%) of study subjects (N = 7) experienced a transient reduction in visual acuity. All three fluoroquinolones were well tolerated and reached levels in the conjunctiva above the MIC(90)s of methicillin-sensitive S. aureus and S. epidermidis for at least 2 hours.