European Journal of Drug Metabolism and Pharmacokinetics

, Volume 6, Issue 1, pp 61–70

On the pharmacokinetics of domperidone in animals and man IV. The pharmacokinetics of intravenous domperidone and its bioavailability in man following intramuscular, oral and rectal administration

Authors

  • J. Heykants
    • Department of Drug Metabolism and PharmacokineticsJanssen Pharmaceutica
    • Medical DepartmentJanssen Pharmaceutica
  • R. Hendriks
    • Department of Drug Metabolism and PharmacokineticsJanssen Pharmaceutica
    • Medical DepartmentJanssen Pharmaceutica
  • W. Meuldermans
    • Department of Drug Metabolism and PharmacokineticsJanssen Pharmaceutica
    • Medical DepartmentJanssen Pharmaceutica
  • M. Michiels
    • Department of Drug Metabolism and PharmacokineticsJanssen Pharmaceutica
    • Medical DepartmentJanssen Pharmaceutica
  • H. Scheygrond
    • Department of Drug Metabolism and PharmacokineticsJanssen Pharmaceutica
    • Medical DepartmentJanssen Pharmaceutica
  • H. Reyntjens
    • Department of Drug Metabolism and PharmacokineticsJanssen Pharmaceutica
    • Medical DepartmentJanssen Pharmaceutica
Original Papers

DOI: 10.1007/BF03189516

Cite this article as:
Heykants, J., Hendriks, R., Meuldermans, W. et al. European Journal of Drug Metabolism and Pharmacokinetics (1981) 6: 61. doi:10.1007/BF03189516

Summary

The pharmacokinetics and bioavailability of domperidone, a novel gastrokinetic, were studied in healthy male subjects by comparing plasma concentrations and urinary excretion following intravenous, intramuscular, oral and rectal administration. Two oral dosage forms were studied: 10-mg tablets and a 10-mg/ml oral solution. The influence of a meal on the oral bioavailability and the dose-proportionality were also investigated.

Plasma levels of intravenous domperidone could be described by a three-compartment model with a rapid distribution of 40% of the dose to as «shallow» peripheral compartment. The final elimination half-life was 7.5 hours. Peak plasma levels were reached within 30 minutes following intramuscular and oral administration and at 1–4 hours following rectal administration. Since domperidone showed an extensive first-pass elimination, AUC-values -a measure for the bioavailability- were consider-ably lower after oral than after parenteral administration. Equal oral and rectal doses gave a similar bioavailability. AUC-values increased proportionally with the dose over a 10–60 mg range. Cumulative urinary excretion of unchanged domperidone was proportional to corresponding AUC-values.

The bioavailability was discussed in the light of the therapeutic results.

Key words

domperidonegastrokineticpharmacokineticsbioavailabilityman
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Copyright information

© Springer-Verlag 1981