[Pharmacokinetics of topically applied fluconazole in the rabbit eye].
OBJECTIVE
To observe the penetration of 0.5% fluconazole (FCZ) into the corneas and aqueous humors of New Zealand white rabbits following its topical application.


METHODS
The rabbit corneas and aqueous humors were obtained and quantified at different times after topically applying 0.5% FCZ to the rabbit eyes. The drug levels were assayed by high performance liquid chromatography (HPLC). The pharmacokinetic parameters were calculated with nonlinear least square method by the computer.


RESULTS
FCZ can rapidly penetrate into rabbit corneas. Peak corneal levels occurred essentially immediately at 2 min in the corneas (15.20 +/- 1.95) microgram/g and at 15 min after application in the aqueous (2.39 +/- 0.92 mg/L). The permeability of the corneal epithelial barrier (Kep) was 1.06 x 10(-5). The half-life (t(l/2)) of the cornea was 63.96 min, and that of the aqueous humor was 42.14 min.


CONCLUSIONS
Topical fluconazole can be used as a topical antifungal agent to treat keratitis and needs further evaluation for treating fungal endophthalmitis.
Zhang
Junjie
J
Henan Institute of Ophthalmology, Zhengzhou 450003, China. zhangjj05@sina.com
Xie
Leike
L
Chen
Zuji
Z
Zhang
Qiang
Q
D000818:Animals; D000935:Antifungal Agents / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001082:Aqueous Humor / Q000378:metabolism*; D003315:Cornea / Q000378:metabolism*; D019573:Epithelium, Corneal / Q000378:metabolism*; D005260:Female; D015725:Fluconazole / Q000493:pharmacokinetics* / Q000627:therapeutic use; D007634:Keratitis / Q000188:drug therapy; D008297:Male; D023421:Models, Animal; D011817:Rabbits
D000935:Antifungal Agents; D015725:Fluconazole