Pharmacokinetics of terbinafine in the rabbit ocular tissues after topical administration.
OBJECTIVE
To determine the distribution of terbinafine in the cornea and aqueous humor after topical administration.


METHODS
A corn oil ointment of terbinafine 0.2% (resolved in sterile corn oil) was applied to the conjunctival sac of albino rabbits twice (with a 5-min interval). The concentration of terbinafine was determined with high-performance liquid chromatography (HPLC) 5, 15, 30, 60, 120 and 240 min after administration of terbinafine.


RESULTS
After topical administration, the concentration of terbinafine increased gradually, reached a peak (1.39 microg/ml at 30 min in the cornea and 82.9 ng/ml at 30 min in aqueous humor, respectively) and then decreased. The concentration was 0.18 microg/g at 240 min in the cornea, but terbinafine could not be tested at 120 min in aqueous humor.


CONCLUSIONS
Topical ophthalmic terbinafine 0.2% could penetrate into the cornea and aqueous humor at concentrations adequate for inhibition of fungus.
Sun
X G
XG
Department of Ocular Microbiology, Beijing Institute of Ophthalmology, Beijing Tongren Hospital, Capital University of Medical Sciences, Beijing, China. sunxuguang@yahoo.com
Wang
Z X
ZX
Wang
Z Q
ZQ
Deng
S J
SJ
Li
R
R
Luo
S Y
SY
Wu
Y Y
YY
D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000493:pharmacokinetics*; D001082:Aqueous Humor / Q000378:metabolism*; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D003315:Cornea / Q000378:metabolism*; D009281:Naphthalenes / Q000493:pharmacokinetics*; D011817:Rabbits; D000077291:Terbinafine; D014018:Tissue Distribution
D000935:Antifungal Agents; D009281:Naphthalenes; D000077291:Terbinafine