性别对艾普拉唑的药代动力学和药效学的影响  

Gender differences in pharmacokinetics and pharmacodynamics of ilaprazole

作　　者：周银平 刘春艳[1] 刘雪梅[1] 徐雯[1] 邵凤[2] 胡海棠[3] 侯雪梅[3] 江骥[1] 王洪允[1] ZHOU Yin-ping;LIU Chun-yan;LIU Xue-mei;XU Wen;SHAO Feng;HU Hai-tang;HOU Xue-mei;JIANG Ji;WANG Hong-yun(Clinical Pharmacology Research Center,Peking Union Medical College Hospital,Peking Union Medical College and Chinese Academy of Medical Sciences,Beijing 100730,China;Phase I Clinical Laboratory,People's Hospital of Jiangsu Province,Nanjing 210029,Jiangsu Province,China;Medical Clinical Research Center,Livzon Group,Zhuhai 519020,Guangdong Province,China)

机构地区：[1]中国医学科学院北京协和医院临床药理中心,北京100730 [2]江苏省人民医院Ⅰ期临床研究室,江苏南京210029 [3]丽珠集团医学临床研究中心,广东珠海519020

出　　处：《中国临床药理学杂志》2020年第8期994-998,共5页The Chinese Journal of Clinical Pharmacology

基　　金：国家“十三五”重大新药创制专项子课题资助项目(2019ZX09734001-001)。

摘　　要：目的评价性别对艾普拉唑的药代动力学和药效学的影响。方法整合不同剂量注射用艾普拉唑在男性和女性受试者中的药代动力学和药效学数据,用剂量归一化、体重校正、方差分析等处理方法分析性别的潜在影响。结果在药代动力学方面,给药不同剂量(5,10和20 mg)艾普拉唑钠男女受试者的内在清除率分别为(3627.06±986.01),(3305.23±947.62),(3532.19±840.13)mL·h^-1和(2636.25±739.45),(2739.25±910.40),(2590.67±584.09)mL·h^-1,差异均有统计学意义(均P<0.05),但AUC和Cmax差异均无统计学意义(均P>0.05)。在药效学方面,5,10和20 mg剂量组女性受试者胃pH值-时间曲线下面积(AUEC0-24 h)分别为(137.17±25.43),(142.74±19.11),(156.98±22.4),虽然高于男性的(102.61±37.4),(127.58±27.22),(145.32±25.51),差异均无统计学意义(均P>0.05)。结论性别对艾普拉唑的药代动力学有一定影响,但是对药效学没有显著影响。Objective To evaluate gender effect on the pharmacokine-tics and pharmacodynamics of ilaprazole.Methods The pharmacokine-tic and pharmacodynamics study data of intravenous ilaprazole of male and female subjects were combined.The effect of gender was evaluated by various methods including dose and body weight correction and ana-lysis of variance.Results In terms of pharmacokinetics,the internal clearance rates of male and female subjects with different doses of ilaprazole sodium(5 mg 10 and 20 mg)were(3627.06±986.01),(3305.23±947.62),(3532.19±840.13)mL·h^-1 and(2636.25±739.45),(2739.25±910.40),(2590.67±584.09)mL·h^-1 with significant differences between male and female(all P<0.05),but there were no significant differences in AUC and Cmax(all P>0.05).In terms of pharmacodynamics,the area under the gastric pH value-time curve(AUEC0-24 h)of female subjects in 5,10 and 20 mg groups were(137.17±25.43),(142.74±19.11),(156.98±22.4),which was higher than that in men(102.61±37.4),(127.58±27.22),(145.32±25.51),but there were no significant differences(all P>0.05).Conclusion The pharmacokinetics of ilaprazole was somehow affected by gender,however the gender effect on the pharmacodynamics could be ignored.

关 键 词：艾普拉唑 性别 药代动力学 药效学 

分 类 号：R975[医药卫生—药品]