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细胞色素P4502C9基因多态性对健康人体内格列喹酮药代动力学的影响
引用本文:熊晓敏,曾彩雯,严非,熊玉卿,夏春华. 细胞色素P4502C9基因多态性对健康人体内格列喹酮药代动力学的影响[J]. 中国临床药理学杂志, 2011, 27(10)
作者姓名:熊晓敏  曾彩雯  严非  熊玉卿  夏春华
作者单位:1. 江西护理职业技术学院,南昌,330201
2. 南昌大学临床药理研究所,南昌,330006
基金项目:国家十一五重大新药创制专项基金资助项目(2009ZX09309-003)
摘    要:目的研究细胞色素CYP2C9基因多态性对中国人体内格列喹酮药物代谢动力学的影响。方法用RELP-PCR方法对38名健康受试者进行CYP2C9基因多态性检测,并按不同CYP2C9基因型进行分组,用高效液相色谱-荧光检测法测定受试者体内格列喹酮的血药浓度并计算相应的药代动力学参数,比较不同基因型受试者间药代动力学参数的差异。结果在38名健康受试者中,发现3名CYP2C9*1/*3杂合突变型个体与35名CYP2C9*1/*1野生型个体;未发现CYP2C9*3/*3纯合突变型个体。随机抽取的17名野生型个体与3名杂合突变型个体在给予格列喹酮60 mg后,发现杂合突变型个体AUC0-t、AUC0-∞、CL/F分别相当于野生型个体的1.854,1.787,0.554倍。结论 CYP2C9基因多态性对格列喹酮的药代动力学有显著影响,CYP2C9*1/*3突变型个体临床应适当调整给药剂量。

关 键 词:细胞色素P4502C9  基因多态性  格列喹酮  药代动力学  

Influence of CYP2C9 polymorphism on the pharmacokinetics of gliquidone in Chinese healthy subjects
XIONG Xiao-min,ZENG Cai-wen,YAN Fei,XIONG Yu-qing,XIA Chun-hua. Influence of CYP2C9 polymorphism on the pharmacokinetics of gliquidone in Chinese healthy subjects[J]. The Chinese Journal of Clinical Pharmacology, 2011, 27(10)
Authors:XIONG Xiao-min  ZENG Cai-wen  YAN Fei  XIONG Yu-qing  XIA Chun-hua
Affiliation:XIONG Xiao-min,ZENG Cai-wen,YAN Fei,XIONG Yu-qing,XIA Chun-hua (Clinical Pharmacology Institute of Nanchang University,Nanchang 330006,China)
Abstract:Objective To investigate the influence of cytochrome P4502C9 polymorphism on the pharmacokinetics of gliquidone in Chinese healthy subjects.Methods Thirty-eight healthy subjects were genotyped by using RELP-PCR method and grouped according to the different CYP2C9 genotype.After oral administration of 60 mg gliquidone,the plasma concentrations of gliquidone in subjects were determined by HPLC-fluorescence detection method.The pharmacokinetic parameters of gliquidone were calculated and compared between diffe...
Keywords:cytochrome P4502C9  polymorphism  gliquidone  pharmacokinetics  
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