湖北科技学院学报（医学版）2025，Vol.39Issue(2)：98-102,106,6.DOI:10.16751/j.cnki.2095-4646.2024102909
CYP2C19基因多态性对奥美拉唑药代动力学影响
Effect of CYP2C19 Genetic Polymorphisms on the Pharmacokinetics of Omeprazole
摘要
Abstract
Objective To investigate the influence of different CYP2C19 genotypes on the pharmacokinetics of omeprazole magnesium enteric-coated tablets in Chinese adult subjects.Methods A total of 32 healthy Chinese adult participants were recrui-ted for this study.Each subject received a single oral dose of the reference formulation of omeprazole magnesium enteric-coated tab-lets while fasting,followed by genetic testing.The study employed a single-center,randomized,open,single-dose,two-formulation,four-period,two-sequence fully replicated crossover design.Participants were administered either the test formulation(20 mg)or the reference formulation(20mg),and blood samples from those in the fasting state were collected up to 14 hours post-administration.The concentration of omeprazole magnesium in these blood samples was quantified using ultra-performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS).Key pharmacokinetic parameters for omeprazole magnesium were calculated utilizing non-compartmental analysis(NCA module)via Phoenix WinNonlin 8.2 software to assess how different CYP2C19 genotypes affect drug metabolism.Results After administration of the test formulation,Cmax and AUC0-t values of the normal metabolizer group,the intermediate metabolizerer group,and the slow metabolizer group were(286.2±75.7)μg/L,(511.9±198.5)μg·h/L;(542.8±123.6)μg/L,(1075.58±476.21)μg·h/L;(1209.1±165.6)μg/L,(4539.83±1064.55)μg·h/L respectively.There were significant differences among the three groups(P＜0.05).When taking the reference preparation on a fasting basis,,Cmax and AUC0-t values of the normal metabolizer group,the intermediate metabolizerer group,and the slow metabolizer group were(264.1±84.7)μg/L,(545.11±229.8)μg·h/L;(538.7±183.1)μg/L,(1110.66±826.33)μg·h/L;(1234.4±182.1)μg/L,(4308.98±1500.34)μg·h/L,respectively,and there were significant differences among the three groups(P＜0.05).The 90％confidence intervals of the geometric mean ratios of the main pharmacokinetic parameters(,Cmax,AUC0-t,AUC0-∞)of the two preparations were all within 80.00％～125.00％.Conclusion Variability in CYP2C19 gene polymorphisms among individuals re-sults in differences in CYP2C19 enzyme activity and affecting plasma concentrations and overall pharmacokinetic profiles of ome-prazole magnesium enteric-coated tablets in the human body.关键词
奥美拉唑镁/CYP2C19/基因组学/药代动力学/肠溶片Key words
Omeprazole Magnesium/CYP2C19/Genomics/Pharmacokinetics/Enteric-coated Tablets分类
药学引用本文复制引用
朱琦涛,姜敏生,尹咸淼,宋欢,丁峰,甘方良..CYP2C19基因多态性对奥美拉唑药代动力学影响[J].湖北科技学院学报（医学版）,2025,39(2):98-102,106,6.基金项目
咸宁市科技计划社发类研发重点专项(2021SFYF005) （2021SFYF005）
