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Ruth Evans, Frank Bucci; The Pharmacokinetics and Aqueous Humor Penetration of Besifloxacin 0.6% and Moxifloxacin 0.5% in Patients Undergoing Cataract Surgery. Invest. Ophthalmol. Vis. Sci. 2013;54(15):4290. doi: https://doi.org/.
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© ARVO (1962-2015); The Authors (2016-present)
To compare the aqueous penetration and pharmacokinetics of besifloxacin 0.6% and moxifloxacin 0.5% in patients undergoing phacoemulsification.
120 patients participated in a randomized, single center, single-masked, active comparator, parallel group absorption study. Patients were randomized in a 1:1 ratio to receive either BESI (n=60) or MOXI (n=60) to 1 of 4 subgroups. Each pt. was instructed to take 1 drop QID for 3 days prior to their surgery. On the day of surgery, pts. were instructed to use their drops at 1 of 4 prearranged times. Aqueous samples were collected at 1,2,4, or 6 hours following their last drop.
Aqueous concentrations were higher for MOXI when compared to BESI at all time periods. The mean aqueous penetration levels at ONE hour were BESI 49 / MOXI 489 ng/ml (p=0.001). The two hour levels were BESI 55 / MOXI 623 ng/ml (p=0.001). At FOUR hours the levels were BESI 74 / MOXI 331 ng/ml (p=0.01). At SIX hours following the last study drops the levels were BESI 47 / MOXI 329 ng/ml (p=0.005). The calculated mean AUC 1-6 was significantly greater for MOXI (2170.1 +/- 171.1) versus BESI (302.8 +/- 28.3) (p<0.0001). Penetration levels for MOXI peaked at 2 hours, and the 4 & 6 hour levels fell below that achieved at the initial 1 hour time period. Penetration levels for BESI peaked at the 4 hour time period, and the 6 hour level was essentially equal to the initial 1 hour time period.
MOXI 0.5% demonstrated significantly greater aqueous penetration vs. BESI 0.6% at all 4 time intervals studied. The AUC 1-6 for MOXI 0.5% was significantly greater than BESI 0.6%. Data for both penetration AND potency are required to evaluate the efficacy of a topical antibiotic. This study provides valuable information regarding the penetration to the aqueous of BESI vs. MOXI when used topically over time.
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