Pharmacokinetics and tissue penetration of rufloxacin, a long acting quinolone antimicrobial agent

The pharmacokinetics of rufloxacin after a single 400 mg oral dose were studied in eight volunteers, measuring plasma, inflammatory fluid and urine concentrations. Mean peak plasma concentrations of 4.4 mg/L were achieved at a mean time of 1.9 h after administration. The mean plasma elimination half-life was 28.2 h. Mean peak levels in inflammatory fluid reached 3.2 mg/L after 3.5 h, and 30.7% of the dose was eliminated in urine by 96 h. The apparent mean volume of distribution of rufloxacin, at steady state, was 109.5 L. The mean percentage penetration of rufloxacin into the inflammatory exudate, as measured by ratios of AUC0-50 h was 90%.