Corneal penetration into rabbit aqueous humor is comparable between preserved and preservative-free tafluprost

Ophthalmic Res. 2009;41(2):118-22. doi: 10.1159/000192082. Epub 2009 Jan 16.


Background: Some studies have shown that benzalkonium chloride (BAK), a preservative used in antiglaucoma medications, can increase corneal permeability by acting as a penetration enhancer. Tafluprost is a new prostaglandin F(2)(alpha) analog in clinical use for the treatment of ocular hypertension and glaucoma.

Methods: This study evaluated the corneal penetration of preservative-free tafluprost 0.0015% eye drops and tafluprost 0.0015% eye drops preserved with 0.01% BAK into the aqueous humor of rabbits.

Results: After the administration of a single topical dose (30 microl), the maximum concentrations at 45 min of tafluprost acid in aqueous humor were 4.50 ng/ml for preservative-free tafluprost and 3.99 ng/ml for preserved tafluprost. The area under the concentration-time curves from 45 min to 3 h was 5.14 ng h/ml for the preservative-free formulation and 4.54 ng h/ml for the preserved formulation.

Conclusions: These data indicate that BAK does not affect the corneal penetration of tafluprost into the rabbit aqueous humor.

MeSH terms

  • Animals
  • Antihypertensive Agents / pharmacokinetics*
  • Aqueous Humor / metabolism*
  • Benzalkonium Compounds / pharmacokinetics
  • Biological Availability
  • Cornea / metabolism*
  • Permeability
  • Preservatives, Pharmaceutical / pharmacokinetics
  • Prostaglandins F / pharmacokinetics*
  • Rabbits


  • Antihypertensive Agents
  • Benzalkonium Compounds
  • Preservatives, Pharmaceutical
  • Prostaglandins F
  • tafluprost