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研究中国汉族人群CYP3A4*18B基因多态性的频率,并探讨CYP3A4*18B基因多态性对替硝唑药代动力学的影响.本研究共招募100名来自中国汉族的健康志愿者,采用PCR-RFLP方法检测CYP3A4*18B的基因多态性.选择CYP3A4*1/*1(n=10)野生型受试者和CYP3A4*1/*18B(n=9)突变杂合型受试者进行替硝唑的药代动力学研究.单剂量口服替硝唑片剂后采集72 h内的血样,使用高效液相色谱法测定血浆样本中替硝唑的浓度.发现88名健康志愿者携带CYP3A4*1/*1基因型,12人携带CYP3A4*1/*18B基因型,未发现携带CYP3A4*18B/*18B基因型.CYP3A4*18B等位基因频率为6％.CYP3A4*1/*1基因型和CYP3A4*1/*18B基因型受试者体内的药动学参数分别为:t1/2:(15.92±1.62),(15.77±1.67)h;Cmax:(18.72±3.10),(20.25±3.42) mg/L;tmax(1.50±0.66),(1.45±0.69)h;Vd/F:(55.73±10.66),(51.30±7.75)L;CL/F:(2.44±0.47),(2.26±0.30) L·h;AUC0-∞:(424.40±82.38),(450.53±69.48) mg·h/L.研究发现CYP3A4*18B基因多态性对替硝唑健康志愿者的药代动力学无明显影响.“,”In the present study,we aimed to investigate the frequency of CYP3A4*18B genetic polymorphism in Han Chinese populations,and to assess the effect of the CYP3A4*18B genetic polymorphism on the pharmacokinetics of tinidazole.A total of 100 healthy volunteers from Han nationalities in China were recruited.DNA was extracted from peripheral leukocytes using a standard protocol.A PCR-RFLP method was developed to detect the alleles of CYP3A4*18B.A pharmacokinetic study of tinidazole was then carried out in two groups with CYP3A4*1/*1 (n =10) and CYP3A4*1/*18B (n =9) genotypes.Concentrations of tinidazole were determined using high-performance liquid chromatography in plasma samples that were collected up to 72 h after drug intake.In this study,88 healthy volunteers were found with CYP3A4*1/*1 genotype,and 12 were found with CYP3A4*1/*18B genotype.CYP3A4*18B/*18B were absent from all subjects.The allele frequencies of CYP3A4*18B were 6％.The pharmacokinetic parameters of CYP3A4*1/*1 genotype and CYP3A4*1/*18B genotype in healthy subjects were as follows:t1/2:(15.92±1.62),(15.77±1.67) h;Cmax:(18.72±3.10),(20.25±3.42) mg/L;tmax:(1.50±0.66),(1.45±0.69) h;Vd/F:(55.73±10.66),(51.30±7.75) L;CL/F:(2.44±0.47),(2.26±0.30) L·h;AUC0-∞:(424.40±82.38),(450.53±69.48) mg·h/L.Collectively,the CYP3A4*18B genetic polymorphism did not affect pharmacokinetics oftinidazolein healthy volunteers.