Pharmacokinetics and tolerance of a new fluoroquinolone antimicrobial drug after single oral doses in healthy volunteers.
1. The pharmacokinetics and tolerance of DV-7751a were investigated in healthy male Caucasian volunteers after single oral doses (100, 200, 400 and 800 mg). 2. DV-7751a was rapidly absorbed in the fasted state. The mean maximum concentration in plasma (Cmax) ranged from 0.27 to 1.98 micrograms/ml for the 100-800-mg dose and the mean time to reach Cmax (tmax) ranged from 1.1 to 1.9 h. The terminal half-life ranged from 8.75 to 10.0 h. A good linear correlation (r = 0.974) was found between doses from 100 to 800 mg and the resulting area under the concentration-time curve (AUC). The plasma protein binding of the drug was in the range of 57-65%. 3. Within 48 h, the cumulative urinary excretion of unchanged drug amounted to 22.0-26.8% of the dose administered. Faecal recovery of the drug up to 72 h after the 400-mg dose was about 12% of the dose given. 4. Adverse events thought to be possibly related to the drug included headache, rash, leg cramp, diarrhoea, abdominal pain, CNS depression and dizziness. DV-7751a, however, was well tolerated with no serious adverse events at any doses and all subjects completed the study. No drug crystals were observed in the urine.
Tanaka
M
M
Daiichi Pharmaceutical Co. Ltd., Tokyo, Japan.
Tamura
K
K
Atarashi
S
S
Kubo
Y
Y
Oliver
S D
SD
Bentley
M
M
Hakusui
H
H
D000328:Adult; D000890:Anti-Infective Agents / Q000009:adverse effects* / Q000493:pharmacokinetics*; D001798:Blood Proteins / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D004311:Double-Blind Method; D005243:Feces / Q000737:chemistry; D024841:Fluoroquinolones; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D011485:Protein Binding; D015363:Quinolones / Q000009:adverse effects* / Q000493:pharmacokinetics*
D000890:Anti-Infective Agents; D001798:Blood Proteins; D024841:Fluoroquinolones; D015363:Quinolones; C084755:DV 7751a