阿斯咪唑片剂人体药代动力学和生物利用度的初步研究  

Pharmacokinetics and bioavailability of astemizole tablets

作　　者：刘军保[1] 陈小川[1] 曹崎 杨广德[2] 杨银京 

机构地区：[1]海南医学院药理教研室,海口570102 [2]西安医科大学药学院

出　　处：《中国临床药理学与治疗学杂志》1998年第2期124-126,共3页

摘　　要：目的观察阿斯咪唑片剂的人体药代动力学和生物利用度。方法用放射免疫法测定血浆阿斯咪唑 +去甲阿斯咪唑含量 ,按交叉设计法对国产和进口阿斯咪唑片进行健康中国人体的药物代谢学比较研究 ,并求得相对生物利用度。用3P87软件处理。结果与结论阿斯咪唑的药代动力学呈二室模型。主要药代动力学参数 :国产片:Vd=5.34±1.85L;αT1/2=0.74±0.37h;βT1/2=286.10±220.11h;CL=0.052±0.031ng/ml;Tmax=1.56±1.32h;Cmax=1.04±0.10ng/ml;AUC=262.69±162.18ng/ml·h-1。进口片 :Vd=8.24±2.56L;αT1/2=1.16±0.98h;βT1/2=260.38±260.37h;CL=0.089±0.079ng/ml;Tmax=1.37±0.82h;Cmax=0.93±0.14ng/ml;AUC=250.66±148.05ng/ml·h -1。国产片对进口片的相对生物利用度为127.8 %。Aim and Methods The pharmacokinetics and bioavailability of the domestic and the imported astemizole tablets were studied in 6 Chinese healthy volunteers by radioimmunoassay in a clinical trial of cross_over design. Results The main pharmacokinetic parameters calculated by the practical pharmacokinetics program 87 were as follows: For the domestic product,Vd=5.34±1.85 L;αT1/2=0.74±0.37 h; βT1/2=286.10±220.11 h; CL=0.052±0.031 ng/ml;Tmax=1.56±1.32 h; Cmax=1.04±0.10 ng/ml; AUC=262.69±162.18 ng/ml·h-1.For the imported product,Vd=8.24±2.56 L;αT1 /2=1.16±0.98 h;βT1 /2=260.38±260.37 h; CL=0.089±0.079 ng/ml;Tmax=1.37±0.82 h; Cmax=0.93±0.14 ng/ml; AUC=250.66±148.05 ng/ml·h-1. The relative bioavailability of the domestic tablets was 127.8%.Conclusion No significant pharmacokinetic difference has been found between the domestic and imported astemizole tablets.

关 键 词：阿斯咪唑 片剂 药代动力学 生物利用度 

分 类 号：R976[医药卫生—药品] R969.1[医药卫生—药学]