Pharmacokinetics and bioequivalence of domestic trimetazidine formulations
10.3760/cma.j.issn.0253-3758.2012.12.013
- VernacularTitle:国产盐酸曲美他嗪的药代动力学和生物等效性研究
- Author:
Wen-Fang LIU
1
;
Jing LI
;
Chang-Sheng MA
;
Yang LIN
;
Ke-Xu YANG
;
Wei SUO
;
Wei WU
;
Gui-Ping ZHAO
Author Information
1. 100029,首都医科大学附属北京安贞医院心内科
- Keywords:
Trimetazidine;
Plasma concentration;
Pharmacokinetics
- From:
Chinese Journal of Cardiology
2012;40(12):1041-1044
- CountryChina
- Language:Chinese
-
Abstract:
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:Cmax(70.9 ± 15.3),(66.4 ± 13.8) μg/ml; tmax(1.70 ± 0.72),(1.85 ± 0.55) h; t1/2z(4.70 ±1.75),(4.77 ± 1.96)h; AUC0-24h(481 ± 176),(469 ± 171)μg· h·ml-1; AUC0-∞(511 ±189),(500 ± 188) μg · h · ml-1.The estimated 90％ CIs for the ratio of C and AUC0-24 h were also similar:101.9％-112.5％ and 99.4％-104.9％.The relative bioavailability of domestic formulation was (102.2 ± 8.3) ％.Conclusion The results demostrats that the domestic hydrochloric trimetazidine capsules and imported hydrochloric trimetazidine tablets are bioequivalent.
