Aqueous penetration of moxifloxacin 0.5% ophthalmic solution and besifloxacin 0.6% ophthalmic suspension in cataract surgery patients

J Cataract Refract Surg. 2010 Sep;36(9):1499-502. doi: 10.1016/j.jcrs.2010.04.030.

Abstract

Purpose: To determine the aqueous humor concentrations of moxifloxacin and besifloxacin after routine preoperative topical dosing in patients having cataract surgery.

Setting: Wilmer Eye Institute, Johns Hopkins University, Baltimore, Maryland, USA.

Methods: In this prospective randomized parallel double-masked clinical trial, 1 drop of commercially available moxifloxacin 0.5% ophthalmic solution or besifloxacin 0.6% ophthalmic suspension was administered every 10 minutes for a total of 4 doses beginning 1 hour before routine cataract surgery. Aqueous humor was sampled via the paracentesis, and antibiotic concentrations were determined using validated high-performance liquid chromatography procedures.

Results: The study enrolled 50 patients. The aqueous concentration of the antibiotic agent was detectable in all 23 moxifloxacin samples and in 10 (40%) of the 25 besifloxacin samples (P<.0001, Pearson chi-square test). The mean aqueous concentration in the moxifloxacin samples was 50-fold higher than in the besifloxacin samples (1.6108 microg/mL versus 0.0319 microg/mL) when all samples were included (P<.0001, Wilcoxon test), while the moxifloxacin concentration was 38-fold higher than the besifloxacin concentration (1.6108 microg/mL versus 0.0422 microg/mL) in the samples with detectable antibiotic agent (P<.0001).

Conclusions: After topical preoperative administration, moxifloxacin 0.5% ophthalmic solution had a 38-fold to 50-fold higher concentration in the aqueous humor than besifloxacin 0.6% ophthalmic suspension. Besifloxacin was undetectable in more than half the aqueous humor samples.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Anti-Infective Agents / pharmacokinetics*
  • Aqueous Humor / metabolism*
  • Aza Compounds / pharmacokinetics*
  • Azepines / pharmacokinetics*
  • Cataract Extraction*
  • Chromatography, High Pressure Liquid
  • Cornea / metabolism
  • Double-Blind Method
  • Fluoroquinolones / pharmacokinetics*
  • Humans
  • Middle Aged
  • Moxifloxacin
  • Ophthalmic Solutions / pharmacokinetics*
  • Prospective Studies
  • Quinolines / pharmacokinetics*

Substances

  • Anti-Infective Agents
  • Aza Compounds
  • Azepines
  • Fluoroquinolones
  • Ophthalmic Solutions
  • Quinolines
  • besifloxacin
  • Moxifloxacin