Pharmaceutisch Weekblad

, Volume 9, Issue 3, pp 179–182 | Cite as

Kinetics of rate controlled rectally administered ranitidine to male volunteers

  • H. de Bree
  • A. C. de Boer
Short Communications


Ranitidine hydrochloride solution was given rectally to six healthy volunteers by means of an osmotic pump (Osmet®) at a zero-order rate for 8 h. Quite constant steady-state drug concentrations were achieved in the range of 64–123 ng/ml plasma (meanCss: 100.6 ng/ml). The mean absorption time was 0.45 h (range 0–1.02 h), indicating that absorption was not always instantaneous. It is concluded that the Osmet® system together with the rectal route offer the possibility for achieving steady-state concentrations of ranitidine, enabling the determination of pharmacodynamic effects. In addition, the rectal route can be considered as an alternative to oral and intravenous administration.

Key words

Administration, rectal Osmotic pump Pharmacokinetics Ranitidine 


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  1. 1.
    Misiewicz JJ, Wormsley KG. The Clinical Use of Ranitidine. The second symposium on Ranitidine. Oxford: The Medicine Publishing Foundation, 1981.Google Scholar
  2. 2.
    Roberts CJC. Clinical pharmacokinetics of ranitidine. Clin Pharmacokinet 1984;9:211–21.PubMedGoogle Scholar
  3. 3.
    Okolic Sanhi L, Venuti M, Strazzabosco M, Orlando R, Nassuato G, Jemmolo RN. Oral and intravenous pharmacokinetics of ranitidine in patients with liver cirrhosis. Int J Clin Pharmacol Ther Toxicol 1984;22:329–32.PubMedGoogle Scholar
  4. 4.
    Miller R. Pharmacokinetics and bioavailability of ranitidine in humans. J Pharm Sci 1984;73:1376–9.PubMedGoogle Scholar
  5. 5.
    Mihaly GW, Drummer OH, Marshall A, Smallwood RA, Louis WJ. High pressure liquid chromatographic determination of ranitidine, a new H2-receptor antagonist in plasma and urine. J Pharm Sci 1980;69:1155–7.PubMedGoogle Scholar
  6. 6.
    Eckenhoff B, Theeuwes F, Urquhart J. Osmotically actuated dosage forms for the rate controlled drug delivery. Pharm Technol 1981;5:35–44.Google Scholar
  7. 7.
    Boutagy J, More DG, Munro IA, Shenfield GM. Simultaneous analysis of cimetidine and ranitidine in human plasma by HPLC. J Liq Chromatogr 1984;7:1651–64.Google Scholar
  8. 8.
    Breimer DD, De Leede LGJ, De Boer AG. New drug delivery systems as tools in clinical pharmacology. In: Lemberger L, Reidenberg MM, eds. Proceedings of the 2nd World Conference on Clinical Pharmacology and Therapeutics. Washington: American Society for Pharmacology and Experimental Therapeutics, 1983:431–43.Google Scholar
  9. 9.
    Nelder JH, Mead R. A simplex method for function minimization. Computer J 1965;7:308–13.Google Scholar
  10. 10.
    Marquardt DW. An algorithm for least squares estimation of nonlinear parameters. J Soc Ind Appl Math 1963;11:431–41.Google Scholar
  11. 11.
    Gibaldi M, Perrier D. Pharmacokinetics, Drugs and the Pharmaceutical Sciences. Vol. 15. New York: Marcel Dekker Inc., 1982:409–17.Google Scholar
  12. 12.
    Peden NR, Richards DA, Saunders JHB, et al. Pharmacologically effective plasma concentrations of ranitidine. Lancet 1979;2:199–200.Google Scholar

Copyright information

© Royal Dutch Association for Advancement of Pharmacy 1987

Authors and Affiliations

  • H. de Bree
    • 1
  • A. C. de Boer
    • 1
  1. 1.Division of Pharmacology, Center for Bio-Pharmaceutical SciencesState University of LeidenRA LeidenThe Netherlands

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