Pharmacokinetics and bioequivalence of atorvastatin calcium tablets in healthy male Chinese volunteers
10.3760/cma.j.issn.0253-3758.2012.03.013
- VernacularTitle:阿托伐他汀在中国健康男性志愿者体内的药代动力学及生物等效性
- Author:
Yi SHEN
1
;
Yi-Fan ZHANG
;
Xiao-Yan CHEN
;
Li-Xia GUO
;
Da-Fang ZHONG
Author Information
1. 浙江工业大学
- Keywords:
Atorvastatin;
Pharmacokinetics;
Bioequivalence
- From:
Chinese Journal of Cardiology
2012;40(3):243-247
- CountryChina
- Language:Chinese
-
Abstract:
Objective To compare the bioequivalence and pharmacokinetics of national made and imported atorvastatin in healthy male Chinese volunteers after single oral administration.Methods This randomized sequence,open-label,two-period crossover study with a one-week washout period between doses was performed in 24 fasting healthy Chinese males.They were randomly assigned to receive 20 mg of either the test ( national made) or reference (imported) formulation orally.The blood samples were collected over a 72-hour period.Plasma concentrations of parent atorvastatin (AT),ortho-hydroxy-atorvastatin (o-OAT)and para-hydroxy-atorvastatin (p-OAT) were simultaneously determined using the validated liquid chromatography-tandem mass spectrometry method,the bioequivalence was also evaluated throughout the study.Results The main pharmacokinetic parameters of test and reference formulations were as follows:the values of Cmax for AT were ( 10.6 ± 11.9 ) μg/L and ( 10.6 + 9.8 ) μg/L,t1/2z were ( 11.4 ± 3.9 ) h and ( 11.4 ± 5.3 ) h,AUC0-t were (54.2 ± 37.4) μg · h - 1 · L- 1 and (51.7 ± 34.1 ) μg · h -1 · L- 1,respectively.The values of Cmax for o-OAT were (7.8 ±4.5) μg/L and (7.6 ±4.3) μg/L,t1/2z were (12.3 ±4.2) h and ( 11.9 ± 3.4) h,AUC0-t were (96.8 ± 48.2) μg · h - 1 · L- 1 and (92.3 ± 44.4) μg · h - 1 · L - 1,respectively.The values of Cmax for p-OAT were (0.5 ±+ 0.4 ) μg/L and (0.4 + 0.3 ) μg/L,t1/2z were ( 18.4 + 12.4 ) h and (23.3±17.8) h,AUC0-t were (15.9+12.3) μg· h-1 · L-1 and (13.8+8.11) μg· h-1 · L-1,respectively.The relative bioavailability of AT and o-OAT in test formulation were ( 105.3 ± 20.7 ) ％ and ( 107.8 ±23.2)％,respectively.The 90％ confidence interval of the test/reference geometric mean ratios of AUC0-t for AT and o-OAT were (97.7 - 110.5)％ and (98.3 - 111.3)％,Cmax for AT and o-OAT were (75.8- 114.0)％ and (90.6 -122.9)％,they were all located within the bioequivalence criteria range (80％ -125％ for AUC,and 70％ - 143％ for Cmax ).Conclusion The result demonstrated that two formulations were bioequivalent.
