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Pharmacokinetics and Pharmacodynamics of a Novel Extended‐Release Ciprofloxacin in Healthy Volunteers
Author(s) -
Washington Carla B.,
Hou S. Y. E.,
Campanella Corinne,
Hughes Nicki,
Brown Steven,
Berner Bret
Publication year - 2005
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270005280542
Subject(s) - ciprofloxacin , pharmacokinetics , crossover study , ciprofloxacin hydrochloride , pharmacology , bioavailability , pharmacodynamics , medicine , minimum inhibitory concentration , area under the curve , antibacterial agent , chemistry , antibiotics , biochemistry , alternative medicine , pathology , placebo
Two open‐label, randomized, 2‐way crossover studies (1 single‐dose and 1 steady‐state) were conducted in healthy volunteers to compare the pharmacokinetics and pharmacodynamics of a novel extended‐release ciprofloxacin (ciprofloxacin ER; 500 mg once daily) and immediate‐release ciprofloxacin (ciprofloxacin IR; 250 mg twice daily). For both studies, mean ciprofloxacin maximum concentration (C max ) values after once‐daily ciprofloxacin ER were significantly greater than those after the first daily dose of ciprofloxacin IR ( P < .0001) but were lower than those after the second daily dose of ciprofloxacin IR ( P < .05). The relative bioavailability of ciprofloxacin ER compared to ciprofloxacin IR was 93.8% in the single‐dose study and 97.7% in the steady‐state study. Mean urinary ciprofloxacin concentrations and excretion rates after either treatment were substantially greater than the minimum inhibitory concentrations (MICs) for susceptible uropathogens in both studies. The area under the concentration‐time curve (AUC)/MIC, C max /MIC, amount excreted (Ae)/MIC, and Ae 24 /MIC ratios with ciprofloxacin ER were similar to or slightly greater than with ciprofloxacin IR for all susceptible organisms.