Relative bioavailability of ofloxacin tablets in comparison to oral solution

Single oral doses of solution and tablet preparations of 300 mg ofloxacin were given to 13 healthy male volunteers in an open, randomized crossover study. Concentrations of the unchanged drug were monitored at various times in serum and urine, over 28 hours and 48 hours, respectively. Each dose was followed by a 1-week washout period. Drug concentrations were measured both by a specific high pressure liquid chromatography (HPLC) method and a microbiological assay. A linear distribution independent regression analysis for method comparisons was calculated and good agreement between the two methods was found. Medians of maximum serum concentrations (Cmax) of ofloxacin after oral solution and tablet form were 5.0 mg/l and 3.5 mg/l, respectively. The times to maximal serum concentration (tmax) were 0.5 hr and 1.0 hr, respectively. The lower Cmax and later tmax after the tablet form were both statistically (p less than 0.05) different when compared to the corresponding values after the oral solution. However, the areas under the serum concentration-time curves (AUC0-28), as also the urinary recoveries did not differ significantly, showing that only the speed of absorption, but not the bioavailability of the tablet is changed in comparison to the oral solution form. Long-lasting, clinically relevant urine concentrations of ofloxacin were observed after both forms until the last collecting fraction (36 to 48 hours after medication). General tolerability was good; no side-effects were reported.