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Pharmacokinetics of sparfloxacin (5-amino-l-cyclopropyl-7-(cis-3, 5-dimethyl -1-piperazinyl)-6, 8-difluoro-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid, SP FX), a new synthetic antibacterial agent, was investigated in rats, dogs and monkeys after oral and intravenous administration of 5 mg/kg. The results were as follows :1. SPFX was well absorbed (60-90% of the dose) from the gastrointestinal tract in all species examined.After oral dosing at a dose of 5mg/kg, plasma levels of SPFX in rats, dogs and monkeys reached a peak of 0. 67, 1.32 and 0.45pg/ml, respectively, and decreased with apparent elimination half-lives of 3. 5, 8. 2 and 5. 6h, respectively.2. There were no sex-related differences in the pharmacokinetics of SPFX in rats.3. The pharmacokinetics of SPFX in rats was not affected with its 7-day consecutive administration.4. The plasma concentration-time profile in rats with D-galactosamine-in duced hepatic disorder was in good agreement with that in normal rats.5. In dogs, SPFX was well distributed in many tissues at concentrations exceeding the plasma levels, but was poorly distributed in the central nervous system.6. The glucuronic acid conjugate of SPFX was found together with the unchanged drug in the urine of all species. No metabolites were detected in rat feces.7. Urinary and fecal excretion in rats after oral dosing accounted for 15.8 % and 81.9% of the dose, respectively.A total amount excreted in the urine was 14.3% of the dose in dogs and 17.3% in monkeys.

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