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Clinical Trial
. 2000 Jan;49(1):32-8.
doi: 10.1046/j.1365-2125.2000.00105.x.

The pharmacokinetics of oral fleroxacin and ciprofloxacin in plasma and sputum during acute and chronic dosing

E J Begg  1 , R A Robson, D A Saunders, G G Graham, R C Buttimore, A M Neill, G I Town
Affiliations
Clinical Trial

The pharmacokinetics of oral fleroxacin and ciprofloxacin in plasma and sputum during acute and chronic dosing

E J Begg et al. Br J Clin Pharmacol. 2000 Jan.

Abstract

Aims: To examine the pharmacokinetics of ciprofloxacin and fleroxacin in plasma and sputum of patients with an acute exacerbation of chronic bronchitis or bronchiectasis following the first dose and again during the third day of treatment.

Methods: Twelve patients, aged >35 years, with acute infective exacerbation of bronchitis or bronchiectasis were allocated randomly to treatment with either fleroxacin 400 mg daily or ciprofloxacin 500 mg twice daily in an open, parallel group design. Plasma and sputum were collected during the first and third days of treatment. The time course of concentrations in sputum was modelled assuming that it acted as a negligibly small compartment of distribution.

Results: The mean sputum to plasma ratios of both ciprofloxacin and fleroxacin were approximately 1 on both days 1 and 3. Peak concentrations of ciprofloxacin in sputum were achieved 1.6 (95% CI on mean difference 0.8-2.3) and 1.2 (0.4-1.9) h later than in plasma on day 1 and day 3, respectively (mean difference +/- 95% confidence interval). For fleroxacin, the corresponding delay in time to peak concentrations was less marked and not significant. Fleroxacin accumulated in plasma (accumulation index 1.52+/-0.07) and sputum (accumulation index 1.79+/-0.39) from day 1 to day 3. Accumulation did not occur for ciprofloxacin because the dose interval (12 h) was considerable longer than its half life (3-4 h).

Conclusions: The sputum to plasma ratio of ciprofloxacin and fleroxacin is approximately 1. The time to peak concentrations of ciprofloxacin in sputum is slightly delayed compared with plasma. Fleroxacin accumulates over time in both plasma and sputum consistent with its longer half-life.

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Figures

Figure 1
Figure 1
Time courses of concentrations of ciprofloxacin (a) and fleroxacin (b) in plasma (closed symbols) and sputum (open symbols). Data are shown for patient 1 of the ciprofloxacin group on day 3 and patient 2 of the fleroxacin group on day 1. The curves represent the best fit of equations 1 and 2.
Figure 2
Figure 2
Comparison of sputum to plasma ratios (S/P) calculated by the AUC method (S/P = AUC(plasma)/AUC(plasma)) or the method based on rate constants (S/P = kps.Vc/(Vs.kps)) for ciprofloxacin (a) and fleroxacin (b). The lines of identity are shown. Day 1 (closed symbols), day 3 (open symbols).
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