Food Effect on Bioavailability of Modified-Release Trimetazidine Tablets

Ozbay L., Unal D. Ş., Erol D.

JOURNAL OF CLINICAL PHARMACOLOGY, vol.52, no.10, pp.1535-1539, 2012 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 52 Issue: 10
  • Publication Date: 2012
  • Doi Number: 10.1177/0091270011422813
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.1535-1539
  • Keywords: trimetazidine, bioavailability, food effect, pharmacokinetics, bioequivalence, HUMAN PLASMA, BIOEQUIVALENCE
  • Istanbul University Affiliated: Yes


This study aimed to investigate a food effect on the bioavailability of modified-release (MR) trimetazidine tablets in 36 healthy volunteers. Trimetazidine, an anti-ischemic drug, protects the myocardial cell from the harmful effects of ischemia. The authors investigated the effect of being under a fasting or fed state at the time of drug intake on the bioavailability of trimetazidine 35-mg MR tablets in a randomized, open-label, crossover, 2-arm, 4-period, 2-sequence bioequivalence study design with a 14-day washout period. Plasma concentration of trimetazidine was assayed in timed samples with a validated high-performance liquid chromatography/mass selective detector that had a lower limit of quantification of 2.5 ng/mL. Test and reference formulations gave a mean trimetazidine C-max of 63.26 ng/mL and 69.18 ng/mL for the fasting state and 64.19 ng/mL and 63.11 ng/mL for the fed state, respectively. The AUC(0-tlast) mean of trimetazidine was 726.31 ng.h/mL and 733.01 ng.h/mL for the fasting state and 706.40 ng.h/mL and 691.40 ng.h/mL for the fed state for test/reference formulations. There were no significant differences in pharmacokinetic parameters between the 2 formulations and the fasting/fed states. The authors showed that there is no food effect and no need for a 4-period study to evaluate the bioequivalence of trimetazidine MR tablets.