In vitro dissolution and in vivo bioequivalence evaluation of two brands of trimetazidine tablets

摘要

Trimetazidine is an effective anti-anginal agent and anti-ischaemic effect. The objective of this study was to assess the in vitro dissolution and to evaluate the bioavailability of two brands of trimetazidine dihydrochloride tablets. Prior to the in vivo PKs study, an in vitro comparative dissolution test was performed for 2 oral brands of trimetazidine dihydrochloride tablets (20mg). In vivo PKs study was evaluated in 24 healthy male volunteers after a single dose oral administration in an open, randomized, two-way crossover study with a washout period of 1 week. After an overnight fast, human volunteers were randomly allocated to receive a single dose of either test or reference product. Blood samples were collected over a 24-hour period following drug administration and plasma was analyzed for trimetazidine concentrations using a validated high-performance liquid chromatography assay method. The PK parameters Cmax, AUC0-t, AUC0-∞, tmax, and t1/2 were determined from plasma concentration-time profiles. The 90% confidence intervals for the ratio of log transformed values of Cmax, AUC0-t, and AUCt-∞ of the test product over those of reference were within the acceptable range (0.8-1.25) for bioequivalence. As a result, the 2 trimetazidine formulations are considered bioequivalent and thus could be prescribed interchangeably in the medical practice based on its PK effect and biopharmaceutical performance.