Corneal penetration into rabbit aqueous humor is comparable between preserved and preservative-free tafluprost.
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.
Pellinen
Pertti
P
Santen Oy, Tampere, Finland. pertti.pellinen@santen.fi
Lokkila
Jukka
J
D000818:Animals; D000959:Antihypertensive Agents / Q000493:pharmacokinetics*; D001082:Aqueous Humor / Q000378:metabolism*; D001548:Benzalkonium Compounds / Q000493:pharmacokinetics; D001682:Biological Availability; D003315:Cornea / Q000378:metabolism*; D010539:Permeability; D011310:Preservatives, Pharmaceutical / Q000493:pharmacokinetics; D011460:Prostaglandins F / Q000493:pharmacokinetics*; D011817:Rabbits
D000959:Antihypertensive Agents; D001548:Benzalkonium Compounds; D011310:Preservatives, Pharmaceutical; D011460:Prostaglandins F; C485333:tafluprost