Effects of gene polymorphism on pharmacokinetics of bicalutamide and comparative study on pharmacokinetics of bicalutamide in different formulations
10.13699/j.cnki.1001-6821.2018.09.014
- VernacularTitle:基因多态性对比卡鲁胺药代动力学的影响并比较不同剂型比卡鲁胺的药代动力学特征
- Author:
Yuan-Yuan LI
1
;
Jing WANG
;
Kun WANG
;
Fang TIAN
;
Han-Lu DAI
;
Long-Mei CHENG
;
Yuan-Yuan ZHANG
;
Guo-Fang BI
;
Xiao-Fang WANG
;
Liang WANG
;
Heng-Yan QU
Author Information
1. 中国人民解放军第307医院临床药理学研究室
- Keywords:
bicalutamide;
gene polymorphisms;
HPLC-MS/MS
- From:
The Chinese Journal of Clinical Pharmacology
2018;34(9):1056-1059
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate the effects of ATP-binding cassette sub-family G member 2 (ABCG2) and CYP3A4 gene polymorphisms on the pharmacokinetics of bicalutamide and compare the pharmacokinetic properties of different formulations of bicalutamide (capsules and tablets).Methods The subjects were randomly divided into two groups:a single dose of oral test preparation or reference preparation 50 mg,the high performance liquid chromatography-mass spectrometry was used to determine of plasma concentration of bicalutamide,the Phoenix WinNonlin 6.4 was used to calculate pharmacokinetic parameters,and bioequivalence evaluation.Analysis the effects of ABCG2 gene polymorphisms on the pharmacokinetics of bicalutamide by SPSS.Results The main phannaeokinetie parameters of the bicalutamide in the test and reference preparation were as follows:Cmax were (900.00 ± 159.20) and (902.40 ± 146.10) ng· mL-1;tmax were (26.40 ± 9.60) and (35.30 ± 19.80) h;AUC0-t were (1.96 × 105 ±3.28 × 104) and (2.02 × 105 ±4.84 × 104) ng · h · mL-1;AUC0-∞ were(2.03 × 105 ±3.62 × 104)and(2.11 × 105 ±5.63 × 104)ng · h · mL-1.The 90％ confidence interval of Cmax was 88.93％-111.39％;the 90％ confidence interval of AUC0-t was 85.97％-110.76％,the AUC0-∞ 90％ confidence interval was 85.18％-111.51％.There was a significant difference of AUC0-t between CC,AA and CA group (P ＜0.05) and a significant difference of AUC0-∞ between CC and AA group (P ＜ 0.05).There was significant difference of CL between CC and AA group (P ＜ 0.05).Conclusion The pharmacokinetic properties of the two preparations are similar.
