[Pharmacokinetics and bioequivalence of domestic trimetazidine formulations].
OBJECTIVE
To compare the pharmacokinetics and bioequivalence between domestic hydrochloric trimetazidine capsules and imported hydrochloric trimetazidine tablets in healthy male Chinese volunteers after single oral administration.


METHODS
A single oral dose (test and reference formulations) was given to 24 healthy male Chinese subjects according to an open randomized crossover design. The blood samples were collected before and after administration. Plasma trimetazidine concentration was determined by HPLC-MS/MS. The pharmacokinetic parameters were calculated by WinNonlin Ver 6.2.1 software.


RESULTS
The main pharmacokinetic parameters of domestic and imported formulation of trimetazidine were similar: C(max) (70.9 ± 15.3), (66.4 ± 13.8) µg/ml; t(max) (1.70 ± 0.72), (1.85 ± 0.55) h; t(1/2z) (4.70 ± 1.75), (4.77 ± 1.96) h; AUC(0-24 h) (481 ± 176), (469 ± 171) µg×h×ml(-1); AUC(0-∞) (511 ± 189), (500 ± 188) µg×h×ml(-1). The estimated 90% CIs for the ratio of C(max) and AUC(0-24 h) were also similar: 101.9% - 112.5% and 99.4% - 104.9%. The relative bioavailability of domestic formulation was (102.2 ± 8.3)%.


CONCLUSIONS
The results demonstrates that the domestic hydrochloric trimetazidine capsules and imported hydrochloric trimetazidine tablets are bioequivalent.
Department of Cardiology, Beijing Anzhen Hospital of Capital Medical University, Beijing 100029, China.
Wen-fang
WF
Liu
Jing
J
Li
Chang-sheng
CS
Ma
Yang
Y
Lin
Ke-xu
KX
Yang
Wei
W
Suo
Wei
W
Wu
Gui-ping
GP
Zhao
D000328:Adult; D018592:Cross-Over Studies; D006801:Humans; D008297:Male; D010949:Plasma / Q000737:chemistry / Q000378:metabolism; D013810:Therapeutic Equivalency; D014292:Trimetazidine / Q000097:blood* / Q000493:pharmacokinetics*
D014292:Trimetazidine