[Antibiotic ophthalmic solutions evaluated by pharmacokinetic parameters of maximum concentration in the aqueous].
OBJECTIVE
In order to determine whether the one-component method for calculating drug concentration in the aqueous(AQCmax) is useful for selecting an appropriate ophthalmic solution, 6 general purpose antimicrobial ophthalmic solutions already on the market were investigated.


METHODS
The drugs examined were levofloxacin (LVFX), chloramphenicol(CP), erythromycin lactobionate(EM), micronomicin sulfate(MCR), cefmenoxime hydrochloride(CMX) and disodium sufobenzyl penicillin(SBPC). Fifty microliters of each solutions was instilled into the cul-de-sac of New Zealand White rabbit eyes 3 times at 15-minute intervals. The drug concentrations in(the anterior sac aqueous,: this is wrong) the aqueous humor 10, 30, 60, 120 and 240 minutes after the final instillation were examined by high performance liquid chromatography(HPLC) and/or bioassay. The AQCmax was calculated using the one-compartment method.


RESULTS
The calculated AQCmax was 2.5 micrograms/ml (HPLC method) and 2.28 micrograms/ml (Bioassay Method) for LVFX, 2.17 micrograms/ml for CP, and 0.45 microgram/ml for EM. The AQCmax for CMX, MCR and SBPC could not be calculated by the one-compartment method.


CONCLUSIONS
The AQCmax of LVFX was higher than that of the 2 other general purpose antimicrobial ophthalmic solutions. The AQCmax of these drugs might be a useful parameter for selecting an appropriate ophthalmic solution for the treatment of infected eyes.
Fukuda
Masamichi
M
Department of Ophthalmology, Kanazawa Medical University, 1-1 Daigaku, Uchinada-machi, Kahoku-gun, Ishikawa 920-0293, Japan.
Sasaki
Kazuyuki
K
D000617:Aminoglycosides; D000818:Animals; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics*; D001082:Aqueous Humor / Q000737:chemistry*; D015281:Cefmenoxime / Q000493:pharmacokinetics; D002701:Chloramphenicol / Q000493:pharmacokinetics; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D005839:Gentamicins; D064704:Levofloxacin; D015242:Ofloxacin / Q000493:pharmacokinetics; D009883:Ophthalmic Solutions / Q000493:pharmacokinetics*; D011817:Rabbits; D013408:Sulbenicillin / Q000493:pharmacokinetics
D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D005839:Gentamicins; D009883:Ophthalmic Solutions; C010948:erythromycin lactobionate; D004917:Erythromycin; D002701:Chloramphenicol; D064704:Levofloxacin; D015242:Ofloxacin; D015281:Cefmenoxime; D013408:Sulbenicillin; C037545:micronomicin