Abstract
A single 400-mg oral dose of sparfloxacin was given to each of six healthy male volunteers, and the concentrations of the drug were measured in plasma, cantharides-induced inflammatory fluid, and urine over the subsequent 52 h. The mean peak concentration in plasma of 1.6 micrograms/ml was attained at a mean time of 2.7 h postdose. The mean peak concentration in inflammatory fluid of 1.3 micrograms/ml was attained at a mean time of 5 h postdose. The mean elimination half-life in plasma was 17.6 h, and that in inflammatory fluid was 19.7 h. The overall penetration into inflammatory fluid was 117%. Urinary recovery within the first 52 h postdose was 8.8% of the administered dose. Our results indicate that a once-daily dosage of sparfloxacin should be adequate to treat systemic infections caused by most common bacterial pathogens.
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- Cooper M. A., Andrews J. M., Ashby J. P., Matthews R. S., Wise R. In-vitro activity of sparfloxacin, a new quinolone antimicrobial agent. J Antimicrob Chemother. 1990 Nov;26(5):667–676. doi: 10.1093/jac/26.5.667. [DOI] [PubMed] [Google Scholar]
- Crump B., Wise R., Dent J. Pharmacokinetics and tissue penetration of ciprofloxacin. Antimicrob Agents Chemother. 1983 Nov;24(5):784–786. doi: 10.1128/aac.24.5.784. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gomeni R. PHARM--an interactive graphic program for individual and population pharmacokinetic parameter estimation. Comput Biol Med. 1984;14(1):25–34. doi: 10.1016/0010-4825(84)90017-9. [DOI] [PubMed] [Google Scholar]
- Greenblatt D. J., Kock-Weser J. Drug therapy. Clinical Pharmacokinetics (first of two parts). N Engl J Med. 1975 Oct 2;293(14):702–705. doi: 10.1056/NEJM197510022931406. [DOI] [PubMed] [Google Scholar]
- Nakamura S., Minami A., Nakata K., Kurobe N., Kouno K., Sakaguchi Y., Kashimoto S., Yoshida H., Kojima T., Ohue T. In vitro and in vivo antibacterial activities of AT-4140, a new broad-spectrum quinolone. Antimicrob Agents Chemother. 1989 Aug;33(8):1167–1173. doi: 10.1128/aac.33.8.1167. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Nye K., Shi Y. G., Andrews J. M., Ashby J. P., Wise R. The in-vitro activity, pharmacokinetics and tissue penetration of temafloxacin. J Antimicrob Chemother. 1989 Sep;24(3):415–424. doi: 10.1093/jac/24.3.415. [DOI] [PubMed] [Google Scholar]
- Raoult D., Bres P., Drancourt M., Vestris G. In vitro susceptibilities of Coxiella burnetii, Rickettsia rickettsii, and Rickettsia conorii to the fluoroquinolone sparfloxacin. Antimicrob Agents Chemother. 1991 Jan;35(1):88–91. doi: 10.1128/aac.35.1.88. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wise R., Gillett A. P., Cadge B., Durham S. R., Baker S. The influence of protein binding upon tissue fluid levels of six beta-lactam antibiotics. J Infect Dis. 1980 Jul;142(1):77–82. doi: 10.1093/infdis/142.1.77. [DOI] [PubMed] [Google Scholar]