Human Aqueous Humor Levels Of Gatifloxacin0.3%Eye Gel, Gatifloxacin0.3%and Levofloxacin0.5%Ophthalmic Solution After Topical Dosing

Purpose:Bacterial endophthalmitis is one of the most serious postoperative complications of cataract surgery. The prophylactic and postoperative application of antibiotics is a effective way to prevent and cure endophthalmitis. Fluoroquinolones represented by levofloxacin and gatifloxacin is the common ophthalmic perioperative drugs. The main purpose of this study is to investigate gatifloxacin0.3%eye gel, gatifloxacin0.3%ophthalmic solution and levofloxacin0.5%ophthalmic solution after topical dosing in human eyes,detecting the aqueous drug concentration at different time points, in order to provide therapy proofs for clinical prevention and treatment of bacterial endophthalmitis.Methods:A randomized, double blind and parallel study was applied. Age-related cataract patients(150eyes in150cases) receiving phacoemulsification were randomized into three groups:gatifloxacin0.3%eye gel,50eyes; gatifloxacin0.3%ophthalmic solution,50eyes and levofloxacin0.5%ophthalmic solution,50eyes. Each group was devided into five sub-groups randomly, with10eyes in each sub-group. Gatifloxacin0.3%Eye Gel, gatifloxacin0.3%ophthalmic solution or levofloxacin0.5%ophthalmic solution was applied in each group preoperatively. One drop of antibiotic was administered every15minutes for4doses. During surgery,more than100μl aqueous samples were obtained according to different sub-groups,15.0,30.0,60.0,120.0and180.0min after last drop respectively.100μl aqueous samples were accurately put into test tube by sample injector. Concentration of the antimicrobial agents was determined by the HPLC (high pressure liquidchromatography). Statistical analysis was performed using One-Way ANOVA to detect differences among the antibiotic treatment groups.Results:Humor concentration of gatifloxacin eye gel1.24±0.23,2.00±0.39,2.38±0.70,3.61±1.41,3.47±1.21mg/L was higher than that of levofloxacin ophthalmic solution1.24±0.45,1.91±0.47,2.37±0.76,1.90±0.52,1.26±0.50mg/L and gatifloxacin ophthalmic solution0.88±0.30,1.36±0.41,1.62±0.57,1.57±0.45,1.15±0.31mg/L at the same period after the last drop. The concentration of gatifloxacin eye gel was statistically significant higher than that of gatifloxacin ophthalmic solution at each time point. Meanwhile the concentration of gatifloxacin eye gel was significant higher than that of levofloxacin ophthalmic solution at120.0min and180.0min after the last drop statistically. gatifloxacin eye gel achieved a highest concentration in aqueous humor120.0min after the last drop of every15minutes for4doses while gatifloxacin and levofloxacin ophthalmic solution both achieved a highest concentration in aqueous humor60.0min after the last drop.Conclusions:Topically applied gatifloxacin0.3%eye gel had higher aqueous humor drug level, longer time to reach peak concentration, higher aqueous bioavailability than gatifloxacin0.3%ophthalmic solution and levofloxacin0.5%ophthalmic solution. From the results of this study, gatifloxacin eye gel could be the preference in the topical applied antibiotics to prevent and treat endophthalmitis.