Abstract
Purpose::
Maximum drug concentrations in aqueous (AQCmax) of five fluoroquinolone ophthalmic solutions; MFLX (0.5% moxifloxacin), LVFX (0.5% levofloxacin), GFLX (0.3% gatifloxacin), OFLX (0.3% ofloxacin) and TFLX (0.3% tosufloxacin tosilate), were measured, using albino rabbits.
Methods::
Each solution was instilled three times at fifteen-minute intervals, and drug concentrations in aqueous were measured at 10, 30, 60, 120 and 240 minutes after the last instillation using HPLC.
Results::
The AQCmax of fluoroquinolones were; MFLX (9.04 µg/ml) >LVFX (2.65 µg/ml) >GFLX (1.26 µg/ml) >OFLX (0.89 µg/ml) >TFLX (0.42 µg/ml). On the comparison of AQCmax/MIC (minimum inhibitory concentration), MFLX achieved much higher values than LVFX against Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Enterococcus faecalis and Propionibacterium acnes.
Conclusions::
Based on these findings, MFLX ophthalmic solution is expected to be useful not only for the treatment of ocular infections and prevention of postoperative endophthalmitis but also for inhibition of development of resistance.
Clinical Trial::
www.umin.ac.jp/ctr/index/htm 63459
Keywords: aqueous • antibiotics/antifungals/antiparasitics • anterior chamber