title: Food effect on bioavailability of modified-release trimetazidine tablets.
abstract: This study aimed to investigate a food effect on the bio-availability 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.
authors.affiliation: GLP-GCP Center, Faculty of Pharmacy, Yeditepe University, Istanbul, Turkey. lozbay@yeditepesaglik.com.tr
authors.forename: Latif
authors.initials: L
authors.lastname: Ozbay
authors.forename: Durisehvar Ozer
authors.initials: DO
authors.lastname: Unal
authors.forename: Dilek
authors.initials: D
authors.lastname: Erol
mesh_terms: D000328:Adult; D001682:Biological Availability; D062408:Breakfast; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000493:pharmacokinetics; D005215:Fasting / Q000378:metabolism; D018565:Food-Drug Interactions; D006801:Humans; D008297:Male; D013607:Tablets; D013810:Therapeutic Equivalency; D014292:Trimetazidine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: D003692:Delayed-Action Preparations; D013607:Tablets; D014665:Vasodilator Agents; D014292:Trimetazidine