Penetration of ofloxacin and ciprofloxacin into the aqueous humor of eyes with functioning filtering blebs: a randomized trial

Arch Ophthalmol. 2001 Sep;119(9):1254-7. doi: 10.1001/archopht.119.9.1254.


Objective: To determine concentrations of ofloxacin and ciprofloxacin hydrochloride in aqueous humor after topical or combined topical and oral administration in eyes with filtering blebs.

Design: A prospective, investigator-masked, randomized, controlled comparative study involving 36 eyes of 34 patients with functioning filtering blebs who were to undergo cataract surgery. Treatment groups received either topical ofloxacin or topical ciprofloxacin (instillation of 0.3% ophthalmic solution every 30 minutes for 4 hours before surgery), or a combined topical plus oral regimen (ciprofloxacin hydrochloride, four 100-mg tablets, or ofloxacin, one 400-mg tablet, administered 24-26, 12-14, and 2 hours preceding surgery). The main outcome measure was antibiotic concentration measured by chromatographic separation and mass spectrometry of aqueous samples obtained during surgery.

Results: Topical antibiotic treatment yielded mean concentrations of ofloxacin, 0.75 microg/mL, and ciprofloxacin, 0.21 microg/mL, in aqueous. With combined topical and oral therapy, significantly more ofloxacin was measured than ciprofloxacin (3.84 microg/mL vs 0.35 microg/mL [P<.001]). The combination regimen produced significantly greater ofloxacin levels than did topical therapy alone (P =.007).

Conclusions: Ofloxacin penetrates better than ciprofloxacin into the aqueous of eyes with filtering blebs, particularly after combined topical and oral administration, by which ofloxacin reaches more than a 10-fold greater concentration than does ciprofloxacin. Combined topical and oral therapy with ofloxacin may be beneficial in the treatment of bleb-associated infections.

Publication types

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

MeSH terms

  • Administration, Oral
  • Administration, Topical
  • Adult
  • Aged
  • Aged, 80 and over
  • Anti-Infective Agents / pharmacokinetics*
  • Aqueous Humor / metabolism*
  • Biological Availability
  • Chromatography, High Pressure Liquid
  • Ciprofloxacin / pharmacokinetics*
  • Drug Therapy, Combination
  • Female
  • Filtering Surgery*
  • Gas Chromatography-Mass Spectrometry
  • Humans
  • Male
  • Middle Aged
  • Ofloxacin / pharmacokinetics*
  • Ophthalmic Solutions
  • Prospective Studies


  • Anti-Infective Agents
  • Ophthalmic Solutions
  • Ciprofloxacin
  • Ofloxacin