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Plasma and urine concentrations of flumequine and its microbiologically active metabolite, 7-hydroxyflumequine, were determined in healthy subjects following single oral doses of 400, 800, and 1200 mg of flumequine, and following multiple oral doses of 800 mg given four-times daily. After administration of the single oral doses, antimicrobial levels in plasma and urine were rapidly attained, were proportional to the dose given, and were maintained for 12 to 24 h. The multiple dosage regimen yielded antimicrobial levels in both plasma and urine that were several-fold higher than the levels required to inhibit the growth of susceptible bacteria. Following both the single and multiple dose regimens, the plasma elimination half-life of flumequine was about 7h. The excretion of 7-hydroxyflumequine in the urine contributed significantly to the antimicrobial activity. [ABSTRACT FROM AUTHOR]

The absorption, biotransformation, and pharmacokinetics of the antiinflammatory drug salicylsalicylic acid (SSA) were studied. Healthy adult males received 1000 mg SSA and 1300 mg aspirin according to a crossover design either as a single oral dose (12 subjects) or three times a day for five days (4 subjects). A newly developed, high-pressure liquid chromatographic assay permitted selective, direct measurement of SSA in the presence of high concentrations of salicylic acid, one of its metabolites. Following a single dose, SSA was promptly absorbed (mean time to peak level 1.5 hour) and was eliminated from plasma with a mean half-life of 1.1 hour. Less than 1 per cent was excreted in the urine as unchanged SSA. SSA did not accumulate in the plasma during multiple dosing. Plasma levels of salicylic acid following single and multiple doses of SSA indicate that SSA is extensively hydrolyzed to salicylic acid in the body. The slightly lower levels of salicylic acid after SSA than after aspirin may reflect direct biotransformation of some of the SSA to an SSA conjugate, without hydrolysis to salicylic acid. [ABSTRACT FROM AUTHOR]