Bioavailability of ciprofloxacin and fleroxacin : Results of a preliminary investigation in healthy adult Nigerian male volunteers

• Published in: Biological & pharmaceutical bulletin 2000, Vol.23 (8), p.968-972
• Main Authors: CHUKWUANI, Chinyere M, COKER, Herbert Alexander, ODUOLA, Ayoade M. J, SOWUNMI, Akin, IFUDU, Ndu David
• Format: Article
• Language: English
• Subjects: Adult; Anti-Infective Agents - blood; Anti-Infective Agents - pharmacokinetics; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Area Under Curve; Biological and medical sciences; Biological Availability; Ciprofloxacin - blood; Ciprofloxacin - pharmacokinetics; Fleroxacin - blood; Fleroxacin - pharmacokinetics; Humans; Male; Medical sciences; Pharmacology. Drug treatments; Reference Values
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.23.968

The absolute bioavailability (BA) of ciprofloxacin and fleroxacin were evaluated in 19 adult Nigerian male volunteers. Subjects meeting the selection criteria were randomized to receive treatment either with fleroxacin (200 mg-i.v. and 200 mg oral dose) or ciprofloxacin (200 mg-i.v. and 250 mg oral dose). The i.v./oral or oral/i.v. switch was made after a one week washout period. Blood and urine samples were collected at pre-determined time intervals over a 72 h period for analysis of drug levels. Following intravenous administration the maximum serum concentration (Cmax) was 2.7+/-1.06mg/l for ciprofioxacin and 0.99+/-0.41 mg/l for fleroxacin; the area under the blood level curve (AUC) was 8.82+/-3.19 mg x h/l with ciprofloxacin and 8.52+/-3.83 mg x h/l with fleroxacin. Following oral administration the Cmax was 1.52+/-0.94 mg/l with ciprofloxacin and 0.57+/-0.08 mg/l with fleroxacin; the AUC was 9.87+/-4.10 and 7.55+/-1.42 mg x h/l, respectively. The absolute BA following oral administration was found to be 0.79+/-0.47 for ciprofloxacin and 1.01+/-0.78 for fleroxacin. When these BA results were corrected for renal clearance [Cl(r)] and elimination half-life (t1/2) the values were reduced to 0.37+/-0.17 and 0.31+/-0.18, respectively, for ciprofloxacin and 0.53+/-0.23 and 0.99+/-0.38, respectively, for fleroxacin. Only 38% with ciprofloxacin and 59% with fieroxacin, of the administered dose, was excreted unchanged following oral administration. More work, however, needs to be done on ciprofloxacin to support and/or confirm the above findings. Fleroxacin, on the one hand, exhibited a different trend from that observed in the literature with respect to Cmax and AUC where the values observed in this study were 3--4 fold lower than expected following identical doses, whilst on the other hand the observed BA profile in this study was consistent with literature trends.