Pharmacokinetics of Levofloxacin Lactate Eye-drops in Aqueous Humor of Rabbits / 中国药房

ABSTRACT

OBJECTIVE:To measure the concentrations of levofloxacin in aqueous humor after a single eye dripping of drug and calculate the pharmacokinetic parameters.METHODS:32 rabbits were divided into 8 groups.The rabbit eyeballs were enucleated to make a collection of aqueous humor at 0.125,0.25,0.5,0.75,1.0,2.0,3.0 and 4.0 hours after dripping.All measurements were performed with HPLC.RESULTS:In aqueous humor,Tmax:0.940h,Cmax:0.592?g/ml,T1/2(Ka):0.479h,T1/2 (Ke)0.919h.By using 3p87 pharmacokinetic program,the concentration-time curves were fitted as one-compartment op_en model.CONCLUSION:All the concentrations of levofloxacin at different times after dripping in aqueous humor exceeded the minimum inhibitory concentration for 90%(MIC90)of most bacterial pathogens.These results show that levofloxacin lactate eye-drops may be an effective antimicrobial agent for the treatment and prevention of intraocular infections as well as other ocular infections.