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J.P. McCulley, G. Surratt, W. Shine; 4th Generation Fluoroquinolone Penetration into Aqueous Humor in Humans . Invest. Ophthalmol. Vis. Sci. 2004;45(13):4927.
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Purpose: To compare directly penetration of two 4th generation fluoroquinolones (FQ) [moxifloxacin and gatifloxacin], into aqueous humor (AH) in humans after topical application and to published levels for 2nd and 3rd generation FQs. Methods: Patients scheduled for routine phacoemulsification and IOL insertion who were otherwise without ocular disease, were given, in a double masked fashion, either commercial moxifloxacin 0.5% (VigamoxTM) or gatifloxacin 0.3% (ZymarTM) to use q.i.d. the day before surgery and one hour prior to the surgical entry into the anterior chamber on the day of surgery. AH samples were taken and chromatographically analyzed by HPLC. AH FQ concentration was calculated by peak comparison to a known concentration peak for ciprofloxacin which was run as an internal standard. These were compared to published concentration of other available FQs. Results: Moxifloxacin AH concentration was 2.01 Fg/ml and gatifloxacin was 1.02 Fg/ml. Published values after q.i.d. dosing for ciprofloxacin 0.3% are 0.07 Fg/ml, levofloxacin 0.5% are 0.28 Fg/ml but are not available for ofloxacin with q.i.d. dosing. Conclusions: AH antibiotic concentration achieved at the time of cataract surgery after topical application serves as an effective surrogate for what can be achieved with typical post–operative topical dosing, e.g. q.i.d. Both 4th generation FQs achieved superior AH concentration after q.i.d. dosing compared to prior generation FQs with moxifloxacin achieving twice the concentration of gatifloxacin. The superior and clinically significant penetration of moxifloxacin into the AH can be partially attributed to its greater solubility at neutral pH and greater concentration in the commercial preparation.
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