Pharmacokinetics of chlorhexidine gluconate 0.02% in the rabbit cornea.
OBJECTIVE
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.
Xuguang
Sun
S
Department Ocular Microbiology, Beijing Institute of Ophthalmology, Beijing Tongren Hospital and Capital University of Medical Science, Beijing, China. sunxuguang@yahoo.com
Yanchuang
Liang
L
Feng
Zhang
Z
Shiyun
Luo
L
Xiaotang
Yin
Y
D000287:Administration, Topical; D000818:Animals; D000891:Anti-Infective Agents, Local / Q000493:pharmacokinetics*; D002710:Chlorhexidine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D003315:Cornea / Q000378:metabolism*; D009883:Ophthalmic Solutions / Q000493:pharmacokinetics; D011817:Rabbits; D014018:Tissue Distribution
D000891:Anti-Infective Agents, Local; D009883:Ophthalmic Solutions; C010882:chlorhexidine gluconate; D002710:Chlorhexidine