Pharmacokinetics and inflammatory fluid penetration of sparfloxacin.
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.
Johnson
J H
JH
Department of Microbiology, Dudley Road Hospital, Birmingham, United Kingdom.
Cooper
M A
MA
Andrews
J M
JM
Wise
R
R
D000284:Administration, Oral; D000328:Adult; D001768:Blister / Q000097:blood / Q000139:chemically induced / Q000378:metabolism*; D005122:Exudates and Transudates / Q000378:metabolism*; D024841:Fluoroquinolones; D006801:Humans; D007249:Inflammation / Q000097:blood / Q000378:metabolism*; D007408:Intestinal Absorption; D008297:Male; D015363:Quinolones / Q000097:blood / Q000493:pharmacokinetics*
D024841:Fluoroquinolones; D015363:Quinolones; C061363:sparfloxacin