Comparison of repeated-dose pharmacokinetics of prolonged-release and immediate-release torasemide formulations in healthy young volunteers

M. J. Barbanoj, M. R. Ballester, R. M. Antonijoan, I. Gich, P. Pelagio, S. Gropper, B. Santos, A. Guglietta

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6 Citations (Scopus)

Abstract

The major aim of the study was to compare the pharmacokinetic profile of repeated-dose administration of a prolonged-release (PR) formulation of torasemide with that of an immediate-release (IR) dosage. Sixteen volunteers received one daily dose, on four consecutive days, of 10 mg of torasemide-PR or torasemide-IR in a single-blind, two-treatment, two-period, repeated-dose, cross-over, sequence-randomized clinical trial. Blood samples were collected at various time points on day 1 (single-dose) and on day 4 (repeated-dose) and torasemide concentrations were analysed by LC/MS/MS. Diuretic effect and urine electrolytes were measured. Urinary urgency was subjectively assessed by visual analogue scales. Safety and tolerability were also determined. Based on logged values, bioequivalence parameters, were: on day 1, ratio = 1.07 (90% CI 1.02-1.1), Cmax ratio = 0.69 (90% CI 0.67-0.73); and on day 4, ratio = 1.02 (90% CI 0.98-1.05), Cmax ratio = 0.62 (90% CI 0.55-0.70). PR had longer tmax than IR and showed significantly lower fluctuations of plasma concentrations. Urine evaluations were similar with both formulations, although PR showed a lower urine volume in the first hours post-administration. Episodes of acute urinary urgency occurred later and were subjectively less intensive with PR. No significant adverse events were reported. © 2009 Société Française de Pharmacologie et de Thérapeutique.
Original languageEnglish
Pages (from-to)115-125
JournalFundamental and Clinical Pharmacology
Volume23
Issue number1
DOIs
Publication statusPublished - 1 Feb 2009

Keywords

  • Bioavailability/absorption
  • Healthy volunteers
  • Pharmacokinetics
  • Prolonged-release formulation
  • Repeated-dose
  • Torasemide

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