Antibiotic ophthalmic solutions evaluated by pharmacokinetic parameters of maximum concentration in the aqueous
Abstract
PURPOSE: 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.
CONCLUSION: 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.
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