Influence of food on the oral bioavailability of deramciclane from film-coated tablet in healthy male volunteers

Sándor Drabant, Katalin Balogh Nemes, Viola Horváth, Antal Tolokán, Gyula Grézal, Markku Anttila, Béla Gachályi, Harri Kanerva, Samar Al-Behaisi, George Horvai, Imre Klebovich

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

The effect of a high-fat meal on the oral bioavailability of deramciclane 30 mg tablet was evaluated in 18 healthy male volunteers in a randomised, single dose, two-way crossover study. The drug was administered following an overnight fast or a standardised high-fat breakfast. The plasma concentrations of deramciclane and N-desmethylderamciclane were determined by using a validated HPLC-MS -MS/MS method. An effect of food on the bioavailability was indicated if the 90% confidence interval (CI) for the ratio of geometric means of fed and fasted treatments was not contained in the equivalence limit of 0.8-1.25 for AUC and Cmax. The ratios of the mean Cmax and AUC 0-∞ values of deramciclane were 1.24 (90% CI 1.12-1.38) and 1.31 (90% CI 1.21-1.41) in fed versus fasted subjects, which overlapped but exceeded the equivalence limit. In contrast to the parent compound, the 90% CI of the mean ratios for AUC0-∞ and Cmax of N-desmethylderamciclane were within the predefined range. The 24 and 31% increase in Cmax and AUC0-∞ of deramciclane, respectively, under fed condition is modest and probably has no clinical significance since it is relatively small compared to the inter-individual variability of these parameters.

Original languageEnglish
Pages (from-to)689-695
Number of pages7
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume58
Issue number3
DOIs
Publication statusPublished - Nov 1 2004

Keywords

  • Acid labile
  • Clinical study
  • Deramciclane
  • Food interaction
  • Pharmacokinetics

ASJC Scopus subject areas

  • Biotechnology
  • Pharmaceutical Science

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