性别差异对来曲唑在人体内药代动力学的影响  

Effect of gender difference on the pharmacokinetics of letrozole in healthy volunteers

作　　者：周伶俐[1] 李挺[2] 黄成坷[3] 陈明静 张琦琪 朱光辉[3] ZHOU Ling-li;LI Ting;HUANG Cheng-ke;CHEN Ming-jing;ZHANG Qi-qi;ZHU Guang-hui(Department of Pathology,The Second Affiliated Hospital of Wenzhou Medical University,Wenzhou 325027,Zhejiang Province,China;Clinical Research Unit,The Second Affiliated Hospital of Wenzhou Medical University,Wenzhou 325027,Zhejiang Province,China;Department of Pharmacy,The Second Affiliated Hospital of Wenzhou Medical University,Wenzhou 325027,Zhejiang Province,China)

机构地区：[1]温州医科大学附属第二医院病理科,浙江温州325027 [2]温州医科大学附属第二医院临床研究中心,浙江温州325027 [3]温州医科大学附属第二医院药学部,浙江温州325027

出　　处：《中国临床药理学杂志》2021年第12期1586-1589,共4页The Chinese Journal of Clinical Pharmacology

基　　金：国家重大新药创制科技重大专项资助项目(2020ZX09201002)。

摘　　要：目的研究性别差异对来曲唑在健康志愿者体内药代动力学的影响。方法选择32名健康志愿者(男女各半),单次口服来曲唑片2.5 mg。在服药前和服药后不同时间点采集静脉血,用超高效液相色谱质谱联用法检测来曲唑血药浓度,并计算主要药代动力学参数。结果男、女性单次口服来曲唑2.5mg后的主要药代动力学参数Cmax分别为(31.48±3.97)和(38.79±5.95)ng·mL^(-1),AUC0-t分别为(1545.95±272.36)和(1859.60±412.58)ng·mL^(-1)·h,AUC0-∞分别为(1746.93±375.96)和(2368.81±729.58)ng·mL^(-1)·h,表观分布容积分别为(102.00±19.44)和(114.71±14.22)L,差异均有统计学意义(均P<0.05);tmax分别为(2.22±1.11)和(1.96±0.87)h,t1/2分别为(65.48±27.69)和(68.87±17.52)h,清除率分别为(1.30±0.40)和(1.15±0.31)L·h-1,差异均无统计学意义(均P>0.05)。结论健康志愿者口服来曲唑片后,其体内药代动力学具有性别差异。Objective To study the effect of gender difference on the pharmacokinetics of letrozole in healthy volunteers.Methods A total of32 healthy volunteers(half male and female)were selected to take letrozole tablets 2.5 mg once,orally.Before and after administration,the plasma samples were collected for the detection of drug concentrations by UPLC-MS/MS.Furthermore,the main pharmacokinetic parameters were calculated.Results After a single oral administration of letrozole tablets2.5 mg,the main pharmacokinetic parameters in male and female were calculated and listed as follows:Cmax were(31.48±3.97)and(38.79±5.95)ng·mL^(-1),AUC0-t were(1545.95±272.36)and(1859.60±412.58)ng·mL^(-1)·h,AUC0-∞were(1746.93±375.96)and(2368.81±729.58)ng·mL^(-1)·h,apparent distribution volume were(102.00±19.44)and(114.71±14.22)L.The differences were statistically significant(all P<0.05).Meanwhile,tmax were(2.22±1.11)and(1.96±0.87)h,t1/2were(65.48±27.69)and(68.87±17.52)h,clearance were(1.30±0.40)and(1.15±0.31)L·h-1.The differences were not statistically significant(all P>0.05).Conclusion There were gender differences in pharmacokinetics of letrozole in healthy volunteers.

关 键 词：来曲唑 超高效液相色谱质谱联用法 血药浓度 药代动力学 性别差异 

分 类 号：R979.[医药卫生—药品]