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目的 探讨中国健康受试者细胞色素P(CYP)2B6*6基因多态性对丙泊酚药代动力学和药效学的影响.方法 20例男性健康受试者单次静脉注射丙泊酚2.0mg·kg-1,用HPLC-MS/MS法测定血药浓度;焦磷酸测序法确定受试者基因型;比较不同基因型受试者的药代动力学和药效学参数.结果 20例受试者中,G516T-GG 14例,GS16T-GT/TT6例;A785G-AA 10例,A785G-AG/GG 10例.其中,G516T-GT/TT组和G516T-GG组的意识消失BIS值(BIS-LOC)分别为74.33±7.20和60.43±13.64,差异有统计学意义(P ＜0.05);A785G-AG/GG组和A785G-AA组t1/2β分别为(0.13±0.06)和(0.41±0.38)h,差异有统计学意义(P＜0.05);其他参数Cmax、tmax、AUCo-tAUCo-∞、t1/2α、MRTo-∞、意识消失时间(t-LOC)、BIS-LOC、意识恢复BIS值(BIS-ROC)、达最小BIS值时间(t-BISmin)、最小BIS值(BISmin)、意识消失持续时间(d-LOC)差异均无统计学意义(均P＞0.05).结论 丙泊酚在体内的药代动力学与药效学均与CYP2B6*6基因多态性有关,根据基因型制定个体化给药方案有助于丙泊酚合理使用.“,”Objective To investigate the effects of CYP2B6 * 6 gene polymorphism on the pharmacokinetics and pharmacodynamics of propofol in Chinese healthy subjects.Methods Twenty male healthy subjects were intravenously injected a single dose of 2.0 mg · kg-1 propofol.The plasma concentration of propofol was examined by HPLC-MS/MS method.The genotype of the subjects was determined by pyrosequencing.The pharmacokinetics and pharmacodynamic parameters of different genotype were compared.Results Among the 20 subjects,there were 14 cases of G516T-GG,6 cases of G516T-GT/TT,10 cases of A785G-AA and 10 cases of A785G-AG/GG.The bispectral index-loss of conscious (BIS-LOC) of G516T-GT/TT group and G516T-GG group were 74.33 ± 7.20 and 60.43 ± 13.64,the t1/2β of A785G-AG/GG group and A785G-AA group were (0.13 ±0.06) and (0.41 ±0.38)h,with significant difference (P ＜ 0.05).Other parameters like Cmax,tmax,AUC0-t,AUC0-∞,t1/2α,MRT0-∞,t-LOC,BIS-LOC,BIS-ROC,t-BISmin,BISmin,d-LOC all had no statistical significance (all P ＞ 0.05).Conclusion The pharmacokine-tics and pharmacodynamics of propofol are correlated with the polymorphism of CYP2B6 * 6,individualized dosing regimens based on genotypes contribute to the rational use of propofol.