Abstract
We evaluated the absolute bioavailability of ciprofloxacin, a new quinoline carboxylic acid, in 12 healthy male volunteers. Doses of 200 mg were given to each of the volunteers in a randomized, crossover manner 1 week apart orally and as a 10-min intravenous infusion. Half-lives (mean +/- standard deviation) for the intravenous and oral administration arms were 4.2 +/- 0.77 and 4.11 +/- 0.74 h, respectively. The serum clearance rate averaged 28.5 +/- 4.7 liters/h per 1.73 m2 for the intravenous administration arm. The renal clearance rate accounted for approximately 60% of the corresponding serum clearance rate and was 16.9 +/- 3.0 liters/h per 1.73 m2 for the intravenous arm and 17.0 +/- 2.86 liters/h per 1.73 m2 for the oral administration arm. Absorption was rapid, with peak concentrations in serum occurring at 0.71 +/- 0.15 h. Bioavailability, defined as the ratio of the area under the curve from 0 h to infinity for the oral to the intravenous dose, was 69 +/- 7%. We conclude that ciprofloxacin is rapidly absorbed and reliably bioavailable in these healthy volunteers. Further studies with ciprofloxacin should be undertaken in target patient populations under actual clinical circumstances.
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Selected References
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- D'Argenio D. Z., Schumitzky A. A program package for simulation and parameter estimation in pharmacokinetic systems. Comput Programs Biomed. 1979 Mar;9(2):115–134. doi: 10.1016/0010-468x(79)90025-4. [DOI] [PubMed] [Google Scholar]
- Eliopoulos G. M., Gardella A., Moellering R. C., Jr In vitro activity of ciprofloxacin, a new carboxyquinoline antimicrobial agent. Antimicrob Agents Chemother. 1984 Mar;25(3):331–335. doi: 10.1128/aac.25.3.331. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gonzalez M. A., Moranchel A. H., Duran S., Pichardo A., Magana J. L., Painter B., Forrest A., Drusano G. L. Multiple-dose pharmacokinetics of ciprofloxacin administered intravenously to normal volunteers. Antimicrob Agents Chemother. 1985 Aug;28(2):235–239. doi: 10.1128/aac.28.2.235. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gonzalez M. A., Uribe F., Moisen S. D., Fuster A. P., Selen A., Welling P. G., Painter B. Multiple-dose pharmacokinetics and safety of ciprofloxacin in normal volunteers. Antimicrob Agents Chemother. 1984 Nov;26(5):741–744. doi: 10.1128/aac.26.5.741. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Höffken G., Lode H., Prinzing C., Borner K., Koeppe P. Pharmacokinetics of ciprofloxacin after oral and parenteral administration. Antimicrob Agents Chemother. 1985 Mar;27(3):375–379. doi: 10.1128/aac.27.3.375. [DOI] [PMC free article] [PubMed] [Google Scholar]