Food Effect on Bioavailability of Modified-Release Trimetazidine Tablets


Ozbay L., Unal D. Ş. , Erol D.

JOURNAL OF CLINICAL PHARMACOLOGY, cilt.52, ss.1535-1539, 2012 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 52 Konu: 10
  • Basım Tarihi: 2012
  • Doi Numarası: 10.1177/0091270011422813
  • Dergi Adı: JOURNAL OF CLINICAL PHARMACOLOGY
  • Sayfa Sayıları: ss.1535-1539

Özet

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.