Penetration of topically applied gatifloxacin 0.3%, moxifloxacin 0.5%, and ciprofloxacin 0.3% into the aqueous humor

Ophthalmology. 2005 Mar;112(3):466-9. doi: 10.1016/j.ophtha.2004.09.029.

Abstract

Purpose: To investigate the aqueous penetration of 3 commercially available ophthalmic fluoroquinolones.

Design: Prospective, double-masked, clinical study.

Participants: Fifty-two eyes of 52 patients.

Intervention: Fifty-two patients undergoing cataract surgery were given preoperative topical gatifloxacin 0.3% (Zymar), moxifloxacin 0.5% (Vigamox), or ciprofloxacin 0.3% (Ciloxan). The patients were instructed to use their antibiotic drops 4 times a day for 3 days before surgery. On the day of surgery, patients were given their assigned antibiotic every 15 minutes for 3 doses, 1 hour before their procedure. At the time of surgery, 0.1 ml of aqueous fluid was aspirated from the anterior chamber with an air cannula needle attached to a tuberculin syringe. The aspirate was immediately stored at -70 degrees C.

Main outcome measure: Fluoroquinolone concentrations were determined by reverse-phase high-pressure liquid chromatography assay technique with ultraviolet detection at a wavelength of 275 nm.

Results: Mean aqueous concentration of gatifloxacin in 16 eyes was 0.63 microg/ml (standard deviation [SD], 0.30), moxifloxacin in 14 eyes was 1.31 microg/ml (SD, 0.46), and the mean concentration of ciprofloxacin in 22 eyes was 0.15 microg/ml (SD, 0.11).

Conclusions: Both moxifloxacin (P<0.001) and gatifloxacin (P<0.005) penetrated the aqueous humor at significantly higher levels than ciprofloxacin. Moxifloxacin penetrated into the aqueous humor at significantly higher levels than gatifloxacin (P<0.05). The anterior chamber levels of moxifloxacin and gatifloxacin may be due to the difference in antibiotic concentration.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Anti-Infective Agents / pharmacokinetics*
  • Aqueous Humor / metabolism*
  • Aza Compounds / pharmacokinetics*
  • Biological Availability
  • Cataract Extraction
  • Chromatography, High Pressure Liquid
  • Ciprofloxacin / pharmacokinetics*
  • Double-Blind Method
  • Female
  • Fluoroquinolones / pharmacokinetics*
  • Gatifloxacin
  • Humans
  • Male
  • Middle Aged
  • Moxifloxacin
  • Ophthalmic Solutions / pharmacokinetics
  • Prospective Studies
  • Quinolines / pharmacokinetics*

Substances

  • Anti-Infective Agents
  • Aza Compounds
  • Fluoroquinolones
  • Ophthalmic Solutions
  • Quinolines
  • Ciprofloxacin
  • Gatifloxacin
  • Moxifloxacin