Bioequivalence of azathioprine tablets in healthy volunteers
10.3969/j.issn.1001-6821.2010.01.010
- VernacularTitle:硫唑嘌呤片在健康人体的生物等效性
- Author:
Shao-Jun SHI
1
;
Hui-Juan YAN
;
Yuan-Sheng WAN
;
Hua-Ting CHEN
;
Fan-Dian ZENG
Author Information
1. 华中科技大学同济医学院附属协和医院
- Keywords:
azathioprine;
6-mercaptopurine;
bioequivalenee;
RP-HPLC
- From:
The Chinese Journal of Clinical Pharmacology
2010;26(1):37-39
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the relative bioavailability and bio-equivalence of azathiopfine tablets in healthy volunteers.Methods A single oral dose of 100 mg azathioprine test and reference tablets were given to 20 male healthy volunteers in a randomized crossover study.Plasma metabolite 6-mercaptopurine of azathioprine wag determined by RP-HPLC.The pharmacokinetic parameters and relative bioavailability were calculated with DAS program to evaluate the bioequivalence of the two preparations.Results The concentration-time curves were fitted to a one-compartment open modeL The main pharmacokinetic parameters of azathioprine test and reference tablets were as follows:t_(1/2)were(1.30±0.25)and(1.30±0.34)h;t_(max) were(1.25±0.16)and(1.24±0.21)h;C_(max) were(48.44±17.09)and(52.32±24.37)μg·L~(-1);AUC_(0-1)were(89.49±19.25)and(91.90±25.31)μg·h·L~(-1);AUC_(0-∞)were(96.11±19.74)and(98.36±24.66)μg·h·L~(-1),re-spectively.The relative bioavailability of F_(0-t) and F_(0-∞) were(99.62±15.29)%and(99.39±13.59)%,respectively.Conclusion The two azathiprine preparations are bioequivalent.
