性别因素对依法韦伦在中国健康汉族人体内的药动学的影响  

Effects of gender on pharmacokinetics of efavirenz in Chinese healthy subjects

作　　者：王爱凤[1] 李江峰[2] 张莉蓉[2] 秦玉花[1] 刘银萍[1] 

机构地区：[1]河南省人民医院药学部,河南郑州450003 [2]郑州大学基础医学院药理学教研室,河南郑州450001

出　　处：《中国医院药学杂志》2014年第17期1482-1485,共4页Chinese Journal of Hospital Pharmacy

基　　金：2013年度河南省医学科技攻关计划普通项目;项目批准号201303174

摘　　要：目的:探讨性别对依法韦伦人体内药动学的影响。方法:筛选29名携带CYP2B6*1/*1基因型健康汉族受试者参与该试验(男16例,女13例),服用600 mg依法韦伦片剂后分别于不同时间点定时采血。采用高效液相色谱-质谱联用法分析受试者体内依法韦伦血药浓度,并根据性别进行统计学分析。结果:男性和女性受试者的t1/2分别为(89.87±21.33)h和(95.87±13.38)h,tmax分别为(3.67±1.38)h和(3.38±1.38)h,Cmax分别为(3 674.2±652.3)ng·ml-1和(3 923.6±902.7)ng·ml-1,AUC0-336分别为(145 124.0±32 326.4)h·ng·ml-1和(139 112.6±12 289.8)h·ng·ml-1,AUC0-∞分别为(156 088.8±36 724.4)h·ng·ml-1和(151 064.7±15 123.5)h·ng·ml-1,所考察药动学参数均无统计学差异(P>0.05)。结论:依法韦伦在健康受试者体内的药动学行为无性别差异。OBJECTIVE To explore the impact of gender on pharmacokinetics of efavirenz and provide evidence for reasona-ble clinical administration. METHODS 29 healthy Han volunteers （16 male, 13 female） were enrolled in the study. Each subject received a single dose of 600 mg efavirenz tablets. Blood samples were collected from elbow vein at certain sampling time. The plasma concentrations of efavirenz were determined by high performance liquid chromatography-mass spectrometry （LC- MS）, and the pharmacokinetie parameters were calculated according to gender. RESULTS The h/2 in male and female volunteers were 89. 87 ＋ 21.33 and 95. 87 ＋ 13. 38 h, respectively; the tr were 3. 67 ± 1.38 and 3. 38± 1.38 h, respectively; the Cx were 3 674. 2 ± 652. 3 and 3 923.6 ±902. 7 ng m1-1 , respectively the AUC1-336 were 145 124. 0 ± 32 326. 4 and 139 112. 6 ± 12 289. 8 h.ngom1-1 , respectively; The AUC of them were 156 088. 8± 36 724. 4 and 151 064. 7 ± 15 123. 5 hang.mt-1 , respectively. All the parameters had no significant difference （P〈0. 05）. CONCLUSION Gender does not affect the pharmacokinetic parameters of efavirenz.

关 键 词：性别 依法韦伦 高效液相色谱-质谱联用 药动学 

分 类 号：R945[医药卫生—微生物与生化药学]