Bioequivalence of oral and intravenous ofloxacin after multiple-dose administration to healthy male volunteers. Antimicrob. Agents Chemother

The bioequivalence of oral and intravenous ofloxacin was investigated after the administration of multiple doses of 400 mg every 12 h to 20 healthy male volunteers in a randomized, crossover, open-label study. Ofloxacin concentrations in plasma were evaluated after 4 days of oral or intravenous (1-h infusion) dosing with a 3-day wash-out period between regimens. As expected, delivery to the systemic circulation took slightly longer after the oral dosing (time to maximum concentration of drug in serum of 1.7 h) relative to the 1-h intravenous infusion, but the systemic availabilities of ofloxacin by the two routes of administration were equivalent (area under the concentration-time curve from 0 to 12 h ratio of 95%). Since previous studies have not demonstrated any change in the bioavailability of ofloxacin in infectious disease patients, this study supports the interchange-ability of these dosing regimens. Ofloxacin is a synthetic carboxyquinolone antimicrobial agent with potent broad-spectrum bactericidal activity against gram-positive and gram-negative aerobic and facul-tatively anaerobic bacteria (8). Ofloxacin has been available in the United States as 200-, 300-, and 400-mg tablets since January 1991 and as a 200-, 300-, or 400-mg intravenous (i.v.