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CYP2C9基因多态性对美洛昔康代谢动力学的影响 被引量:1

Effect of CYP2C9 Genetic Polymorphism on the Pharmacokinetics of Meloxicam Metabolism in Chiness Subjects
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摘要 目的研究CYP2C9基因多态性对美洛昔康代谢动力学的影响。方法用焦磷酸测序法对24名健康受试者进行CYP2C9基因多态性检测;用LC-MS-MS法测定美洛昔康的血药浓度;用DAS2.0软件进行房室拟合及药代动力学参数计算,分析美洛昔康人体药代动力学特征,并比较CYP2C9*3突变型和野生型个体对美洛昔康代谢动力学特性的差异。结果 24名受试者中CYP2C9*3等位基因有2种表型(A/A,A/C),其中2名受试者为CYP2C9*3杂合突变型(A/C),其余为野生型(A/A);CYP2C9*3代谢美洛昔康的酶活性A/A﹥A/C。结论 CYP2C9基因多态性对美洛昔康的代谢具有显著影响,CYP2C9*3代谢美洛昔康的酶活性是A/A﹥A/C。检测突变型个体对指导美洛昔康临床个体化用药具有重要意义。 Objective To investigate the effect of CYP2C9 polymorphism on the pharmacokinetics of meloxicam in Chinese healthy subjects.Methods The CYP2C9 genotypes of twenty-four Chinese healthy male subjects were selected by the pyrosequencing method.The subjects were genotyped with CYP2C9*3 wild-type and mutation.HPLC-MS-MS method was used for the determination of meloxicam in plasma.The important pharmacokinetic parameters were caculated by DAS 2.0 software.The pharmacokinetics of meloxicam based on identification of genotypes(CYP2C9*3 wild-type and mutation) was compared.Results Two kinds of CYP2C9*3 phenotype existed in the subjects.CYP2C9* 3(A/A) was found in twenty-two subjects while CYP2C9*3(A/C) in two subjects.For meloxicam,the A/A of CYP2C9*3 alleles was more active than the A/C.Conclusion CYP2C9 genetic polymorphism has significant influence on the pharmacokinetics of meloxicam.A/A is more active than A/C.Pharmacogenomic studies will help rational and individualized medication.
出处 《解放军药学学报》 CAS 2012年第1期24-28,共5页 Pharmaceutical Journal of Chinese People's Liberation Army
关键词 美洛昔康 CYP2C9 等位基因 单核苷酸多态性 基因分型 meloxicam CYP2C9 allele polymorphism genotyping
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  • 1Yoon YR,Shon JH,Kim MK,et al.Frequency of cytochrome P450 2C9 mutantalleles in a Korean population[J].Br J C lin Pharmacol,2001,51 (3):277-280.
  • 2Dupont JM,Tost J,Jammes H,et al.De novo quantitative bisulfite sequencing using the Pyrosequencing technology[J]. Anal Biochem,2004,333(1):119-127.
  • 3Daly AK,Day CP,Aithal GP.CYP2C9 polymorphism and warfarin dose requirements[J].Br J Clin Pharmacol,2002,53(4):408-409.

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