Abstract
1. The absorption of ciprofloxacin from different regions of the human gastrointestinal tract was investigated in four healthy males using a remote-controlled drug delivery device (hf-capsule). 2. Significant differences in AUC were observed in the control study (oral administration of ciprofloxacin solution without the hf-capsule = 100%) and after release of ciprofloxacin in the jejunum (geometric mean: 37%), the ileum (mean: 23%), the ascending colon (mean: 7%) and the descending colon (mean: 5%), whereas tmax showed no difference for any of the absorption sites. Ciprofloxacin release in the stomach resulted in the greatest AUC (mean: 140%). Thus, it is concluded that the main absorption site of ciprofloxacin is the upper gastrointestinal tract, up to the jejunum. 3. Differences in presystemic metabolism of known drug metabolites along the gut could be excluded, as the pattern of urinary recovery of desethylene-, sulpho-, and oxo-ciprofloxacin and the parent compound was similar for all drug release sites.
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- Bergan T., Thorsteinsson S. B., Solberg R., Bjornskau L., Kolstad I. M., Johnsen S. Pharmacokinetics of ciprofloxacin: intravenous and increasing oral doses. Am J Med. 1987 Apr 27;82(4A):97–102. [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]
- Janknegt R. Fluorinated quinolones. A review of their mode of action, antimicrobial activity, pharmacokinetics and clinical efficacy. Pharm Weekbl Sci. 1986 Feb 21;8(1):1–21. doi: 10.1007/BF01975473. [DOI] [PubMed] [Google Scholar]
- Neuman M. Clinical pharmacokinetics of the newer antibacterial 4-quinolones. Clin Pharmacokinet. 1988 Feb;14(2):96–121. doi: 10.2165/00003088-198814020-00003. [DOI] [PubMed] [Google Scholar]
- Nix D. E., Schentag J. J. The quinolones: an overview and comparative appraisal of their pharmacokinetics and pharmacodynamics. J Clin Pharmacol. 1988 Feb;28(2):169–178. doi: 10.1002/j.1552-4604.1988.tb05740.x. [DOI] [PubMed] [Google Scholar]
- Scholl H., Schmidt K., Weber B. Sensitive and selective determination of picogram amounts of ciprofloxacin and its metabolites in biological samples using high-performance liquid chromatography and photothermal post-column derivatization. J Chromatogr. 1987 May 15;416(2):321–330. doi: 10.1016/0378-4347(87)80515-7. [DOI] [PubMed] [Google Scholar]
- Staib A. H., Loew D., Harder S., Graul E. H., Pfab R. Measurement of theophylline absorption from different regions of the gastro-intestinal tract using a remote controlled drug delivery device. Eur J Clin Pharmacol. 1986;30(6):691–697. doi: 10.1007/BF00608217. [DOI] [PubMed] [Google Scholar]