摘要
目的:奥美拉唑作为探针药物分析中国汉族人群细胞色素氧化酶CYP2C19表型多态性。方法:采用HPLC建立了测定体内奥美拉唑及其代谢产物的血药浓度的方法;计算羟化指数(给药后3h的血清奥美拉唑和5’-羟基奥美拉唑的浓度比值,C_(OPZ)/C_(OPZOH)),以C_(OPZ)/C_(OPZOH)阈值为15作为CYP2C19表型分型的指标,对65例中国汉族健康志愿者进行了表型多态性分析。结果:羟化指数C_(OPZ)/C_(OPZOH)在中国汉族人群中呈二态分布,在65例受试者中,8例的C_(OPZ)/C_(OPZOH)大于阈值15,被判定为弱代谢者;57例小于阈值15,被判定为强代谢者;弱代谢者判定率为12.31%,而强代谢者判定率为87.69%。98.46%受试者的表型与其基因型吻合。结论:奥美拉唑是合适的探针药物;中国汉族人群细胞色素氧化酶CYP2C19表型存在多态性。
Objective:To analyze the phenotype polymorphism of cytochrome CYP2C19 in Han nationality using the omeprazole probe. Methods:65 Han volunteers that administered 20 mg omeprazole were phenotyped for the CYP2C19 by measuring the plasma concentrations of omeprazole and hydroxyomeprazole by HPLC. The hydroxylation index (C_(OPZ)/C_(OPZOH) threshold=15——the concentration ratio of omeprazole versus 5'-hydroxy omeprazole in 3 hours) was used as a subphenotype index for the CYP2C19. Results: The hydroxylation index (C(OPZ)/C_(OPZOH)) showed a binary distribution in Han nationality. Of 65 volunteers, 8 (12.31%) had the C_(OPZ)/ C_(OPZOH) of more than 15, suggesting their poor metabolisms, and 57 (87.69%) had the C_(OPZ)/C_(OPZOH) of less than 15, suggesting their extensive metabolisms. 98.46% of these phenotypes were coincident with their corresponding CYP2C19 genotypes. Conclusion:Qmeprazole can be used as a probe drug. The Han nationality have the genotype polymorphism of cytochrome CYP2C19.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2005年第4期461-464,共4页
Chinese Journal of New Drugs
