Pharmacokinetics of chlorhexidine gluconate 0.02% in the rabbit cornea

J Ocul Pharmacol Ther. 2006 Aug;22(4):227-30. doi: 10.1089/jop.2006.22.227.

Abstract

Purpose: The aim of this study was to determine the pharmacokinetic parameters of chlorhexidine gluconate (CHG) in the rabbit cornea.

Methods: Each eye of 16 New Zealand white rabbits were topically instilled with 50 microL of CHG 0.02% eye drops twice with a 5-min interval. Four (4) corneas of 2 rabbits were harvested at each time point. The concentration of CHG in the cornea was determined with high-performance liquid chromatography (HPLC) and 387 software to simulate the pharmacokinetic parameters.

Results: The concentration of CHG in the cornea displayed an open two-compartment model. Tmax was 13.75 min, Cmax 0.713 microg.g1, clearance rate 1.64 microg.g-1.min-1, and t1/2alpha, t1/2beta, and t1/2ka was 2.65, 48.72, and 2.67 min, respectively.

Conclusions: The concentration of CHG in the rabbit cornea could be determined by means of HPLC. The maximum concentration of CHG in the corneal tissue was much higher than the trophozoite minimum amoebicidal concentration (TMAC) in vitro.

MeSH terms

  • Administration, Topical
  • Animals
  • Anti-Infective Agents, Local / pharmacokinetics*
  • Chlorhexidine / analogs & derivatives*
  • Chlorhexidine / pharmacokinetics
  • Chromatography, High Pressure Liquid
  • Cornea / metabolism*
  • Ophthalmic Solutions / pharmacokinetics
  • Rabbits
  • Tissue Distribution

Substances

  • Anti-Infective Agents, Local
  • Ophthalmic Solutions
  • chlorhexidine gluconate
  • Chlorhexidine