Pharmacokinetics and relative bioavailability of clopidogrel bisulfate tablets in Chinese healthy volunteers
10.13699/j.cnki.1001-6821.2015.22.018
- VernacularTitle:硫酸氢氯吡格雷片在中国健康人体的药代动力学和相对生物利用度研究
- Author:
Peng-Fei LI
1
;
Wei-Yue YU
;
Wei-Hang TONG
;
Ping MA
;
Hong-Chuan LIU
;
Cheng WU
;
Li-Hong LIU
Author Information
1. 首都医科大学 附属北京朝阳医院 药事部
- Keywords:
clopidogrel bisulfate tablets;
LC-MS/MS;
pharmacokinetics;
bioequivalence
- From:
The Chinese Journal of Clinical Pharmacology
2015;31(22):2232-2235
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the pharmacokinetics and relative bioavailability of clopidogrel bisulfate tablets in healthy volunteer. Methods A single oral doses of 150 mg ( reference and test) were given to 24 healthy volunteers according to an open randomized crossover design.The concentrations of clopidogrel and its carboxylic acid metabo-lite of reference and test tablets in plasma were determined by LC-MS/MS.Results The pharmacokinetic parameters for clopidogrel of the two preparations were as follow: tmax of test drug and reference drug were (1.03 ±0.36 ), ( 1.11 ±0.41 ) h, Cmax were ( 2.90 ±1.68 ), (3.05 ±1.63) ng·mL-1, t1/2 were (3.50 ±1.19), (3.22 ±0.66) h, AUC0-t were (8.75 ±5.10), (9.26 ±5.36) ng·h·mL-1, AUC0-∞were ( 9.52 ±5.64 ) , ( 9.97 ±5.88 ) ng·h·mL-1 . The relative bioavailability of clopidogrel were (98.40 ±24.30) %.The pharmaco-kinetic parameters for clopidogrel carboxylic acid metabolite of the two preparations were as follow: tmax of test drug and reference drug were (0.98 ±0.72 ), ( 0.91 ±0.40 ) h, Cmax were ( 4799 ±1569 ),(4697 ±1856 ) ng·mL-1 , t1/2 were ( 7.24 ±1.56 ) , ( 7.25 ±1.38 ) h, AUC0-t were ( 13042 ±3845 ) , (13707 ±4007) ng·h·mL-1, AUC0-∞ were (13933 ±4242), (14595 ±4172) ng·h·mL-1.The relative bioavailability of clopidogrel carboxylic acid metabolite were (95.90 ±13.50)%.Conclusion Main pharmacokinetic parameters for clopidogrel and its carboxylic acid metabolite were tested to be bioequivalent.
