Bioavailability of diclofenac potassium at low doses

Research output: Contribution to journalResearch articleContributedpeer-review

Contributors

  • Burkhard Hinz - , Friedrich-Alexander University Erlangen-Nürnberg (Author)
  • Julia Chevts - , Friedrich-Alexander University Erlangen-Nürnberg (Author)
  • Bertold Renner - , Institute of Clinical Pharmacology, Friedrich-Alexander University Erlangen-Nürnberg (Author)
  • Henrike Wuttke - , Friedrich-Alexander University Erlangen-Nürnberg (Author)
  • Thomas Rau - , Friedrich-Alexander University Erlangen-Nürnberg (Author)
  • Andreas Schmidt - , Friedrich-Alexander University Erlangen-Nürnberg (Author)
  • Istvan Szelenyi - , Friedrich-Alexander University Erlangen-Nürnberg (Author)
  • Kay Brune - , Friedrich-Alexander University Erlangen-Nürnberg (Author)
  • Ulrike Werner - , Friedrich-Alexander University Erlangen-Nürnberg (Author)

Abstract

Aim: Diclofenac-K has been recently launched at low oral doses in different countries for over-the-counter use. However, given the considerable first-pass metabolism of diclofenac, the degree of absorption of diclofenac-K at low doses remained to be determined. The aim of this study was to determine the bioavailability of low-dose diclofenac-K. Methods: A randomized, three-way, cross-over study was performed in 10 subjects. Each received diclofenac-K, 22.5 mg via short-term i.v. infusion and orally at single doses of 12.5 mg and 25 mg. Results: Mean (± SD) times to maximal plasma concentration (t max) of diclofenac were 0.48 ± 0.28 h (12.5 mg) and 0.93 ± 0.96 h (25 mg). The absolute bioavailability of diclofenac-K after oral administration did not differ significantly in the 12.5-mg and 25-mg dose group (63.1 ± 12.6% vs. 65.1 ± 19.4%, respectively). The 90% confidence intervals for the AUC and AUCt ratios for the two oral regimes were 82.6, 103.4% (point estimate 92.4%) and 86.2, 112.9% (point estimate 98.6%), respectively. These values were within the acceptance criteria for bioequivalence (80-125%). Conclusions: Our data indicate that diclofenac-K is rapidly and well absorbed at low dose, and are consistent with a rapid onset of action of the drug.

Details

Original languageEnglish
Pages (from-to)80-84
Number of pages5
JournalBritish Journal of Clinical Pharmacology
Volume59
Issue number1
Publication statusPublished - Jan 2005
Peer-reviewedYes

External IDs

PubMed 15606444
ORCID /0000-0003-0845-6793/work/139025231

Keywords

ASJC Scopus subject areas

Keywords

  • Bioavailability, Diclofenac, Pharmacokinetics, Potassium salt