Furosemide pharmacokinetics and pharmacodynamics following gastroretentive dosage form administration to healthy volunteers

Eytan A. Klausner, Eran Lavy, David Stepensky, Eva Cserepes, Miklos Barta, Michael Friedman, Amnon Hoffman

Research output: Contribution to journalArticlepeer-review

53 Scopus citations

Abstract

The objective of this study was to evaluate the pharmacokinetic and pharmacodynamic properties of furosemide following gastroretentive dosage form (GRDF) administration. A furosemide (60 mg) GRDF, releasing the drug during 6 hours in vitro, or an immediate-release tablet was administered to healthy male volunteers (N = 14) in a crossover design. Food and liquid intake were standardized; urine was collected, weighed, and assayed for furosemide and sodium concentrations. Pharmacokinetics of furosemide following the GRDF administration, as compared to the tablet, showed lower Cmax and indicated a prolonged absorption phase leading to longer mean residence time in the stomach. The sustained input of the drug significantly improved diuretic and natriuretic efficiencies during the first 5 hours and thereby increased the total effects measured over 24 hours. The unfolding controlled-release GRDF of furosemide improved the pharmacodynamic actions due to the sustained absorption in the stomach and jejunum, which delayed the body's counteractivity to the drug effect.

Original languageEnglish
Pages (from-to)711-720
Number of pages10
JournalJournal of Clinical Pharmacology
Volume43
Issue number7
DOIs
StatePublished - 1 Jul 2003
Externally publishedYes

Keywords

  • Controlled release
  • Furosemide
  • Gastroretentive
  • Humans
  • Pharmacodynamics
  • Pharmacokinetics

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