Single-dose pharmacokinetics and penetration of BMS 284756 into an inflammatory exudate.
The pharmacokinetics of a single dose of BMS 284756 were determined following oral administration of a 600-mg dose to eight healthy male volunteers. Concentrations of the drug were measured in plasma and a cantharidine-induced inflammatory exudate by a microbiological assay. The mean peak concentration in plasma of 10.4 microg/ml (standard deviation [SD], 1.3 microg/ml) was attained at a mean time of 1.2 h (SD, 0.5 h) after the dose. The penetration into the inflammatory exudate was 82% (SD, 15.7%). A mean peak concentration of 7.2 microg/ml (SD, 2.4 microg/ml) was attained in the inflammatory exudate at 5.3 h (SD, 1.5 h). The elimination half-lives from plasma and inflammatory fluid were 9.8 h (SD, 1.1 h) and 8.5 h (SD, 1.9 h), respectively. The areas under the concentration-time curves for plasma and inflammatory fluid were 96.7 microg x h/ml (SD, 10.3 microg x h/ml) and 77.9 microg x h/ml (SD, 19.2 microg x h/ml), respectively.
Wise
R
R
Department of Medical Microbiology, City Hospital NHS Trust, Birmingham, United Kingdom.
Gee
T
T
Marshall
G
G
Andrews
J M
JM
D000328:Adult; D000890:Anti-Infective Agents / Q000097:blood / Q000493:pharmacokinetics*; D002193:Cantharidin; D024841:Fluoroquinolones; D006801:Humans; D007211:Indoles; D007249:Inflammation / Q000139:chemically induced / Q000378:metabolism*; D008297:Male; D008657:Metabolic Clearance Rate; D015363:Quinolones
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D007211:Indoles; D015363:Quinolones; D002193:Cantharidin; C419689:garenoxacin