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本研究旨在研究CYP3A4* 18基因型对唑吡坦在健康回族人体内的药代动力学行为的影响.采用多聚酶链反应-限制性片段(PCR-RELP)分析,检测200名健康回族志愿者的CYP3A4* 18等位基因.根据CYP3A4* 18等位基因筛选结果,选择CYP3A4* 1/*1,CYP3A4* 1/* 18和CYP3A4* 18/* 18携带者各6名,单剂量口服给予10 mg酒石酸唑吡坦片,分别于给药前和给药后不同时间点采集血浆样品.使用HPLC-FLD法测定唑吡坦血药浓度,采用DAS2.0软件计算药代动力学参数,并采用SPSS17.0软件进行统计分析.结果显示不同基因型受试者唑吡坦的药代动力学行为有明显差异.杂合突变组(*1/*18)和纯合突变组(*18/*18)的唑吡坦Cmax分别为野生组(*1/*1)的0.89 (95％ CI:0.65-1.12)和0.57 (95％ CI:0.47-0.66);AUC0-t分别为*1/*1组的0.74 (95％ CI:0.22-1.26)和0.61 (95％ CI:0.24-0.98).唑吡坦药代动力学参数呈现明显的基因-剂量效应(P＜0.05).本研究证明CYP3A4*18等位基因增强了CYP3A4对唑吡坦的代谢水平,对唑吡坦的人体内药代动力学行为有显著影响.“,”In the present study,we aimed to investigate the effect of CYP3A4* 18 genotype on the pharmacokinetics of zolpidem in healthy Chinese Hui volunteers.Blood samples were collected from volunteers for CYP3A4 genotyping using a polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) assay.A pharmacokinetic study was then carried out in three groups with CYP3A4*1/*1 (n =6),CYP3A4*1/*18 (n =6) and CYP3A4*18/*18 (n =6) genotypes.Plasma levels of zolpidem were determined by PLC-FLD method before and after a single oral dose of 10 mg zolpidem tartrate tablet.Significant differences were observed in the pharmacokinetic parameters ofzolpidem among the three genotype groups (P＜0.05).Compared with the CYP3A4*1/*1 group,the Cmax of zolpidem in *1/*18 and *18/*18 groups (mean,95％ CI) was 0.89 (0.65-1.12) and 0.57 (0.47-0.66),respectively,and the AUC0-ξ in the *1/*18 and *18/*18 groups (mean,95％ CI) was 0.74 (0.22-1.26) and 0.61 (0.24-0.98),respectively.There was a significant trend towards lower Cmax and AUC0-ξ values of zolpidem in individuals with more CYP3A* 18 alleles,suggesting a gene-dosage effect.The study demonstrated that the CYP3A4* 18 allele played an important role in the pharmacokinetics of the zolpidem after oral administration.