阿斯咪唑混悬剂的人体药代动力学  

Study on the pharmacokinetics of astemizole suspensions in healthy volunteers

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3期187-189,共3页

摘　　要：目的比较国产、进口阿斯咪唑混悬剂在健康中国人体的药代动力学。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混悬剂进行健康中国人体的药代动力学的比较,并求相对生物利用度。结果经3P87软件处理 ,阿斯咪唑的药代动力学呈二室模型。主要药代动力学参数 :国产剂 :Vd=6.88±1.36L;αT1/2=4.24±4.06h;βT1/2=170.31±73.80h;CL=0.067±0.023ng/ml;Tpeak=1.00±0.53h;Cmax=1.25±0.17ng/ml;AUC=162.97±48.57ng/ml·h-1。进口片 :Vd=6.40±3.07L;αT1/2=1.31±0.91h;βT1/2=156.02±120.74h;CL=0.079±0.045ng/ml;Tpeak=1.00±0.53h;Cmax=1.08±0.19ng/ml;AUC=173.46±114.66ng/ml·h-1。结论国产、进口阿斯咪唑混悬剂在中国人体的药代动力学参数均未发现明显差异。Aim To compare the pharmacokinetic parameters of the domestic astemizole suspension with those of the imported product in Chinese healthy volunteers. Methods Astemizole and demethylastemizole concentration was measured by radioimmunoassay in a clinical trial of crossover design.Results The main pharmacokinetic parameters of the domestic product calculated by practical pharmacokinetics program 87 were Vd=6.88±1.36 L;αT1/2=4.24±4.06 h;βT1/2=170.31±73.80 h;CL=0.067±0.023 ng/ml;Tpeak=1.00±0.53 h;Cmax=1.25±0.17 ng/ml;AUC=162.97±48.57 ng/ml·h-1,while the parameters of the imported product were Vd=6.40±3.07 L;αT1/2=1.31±0.91 h;βT1/2=156.02±120.74 h;CL=0.079±0.045 ng/ml;Tpeak=1.00±0.53 h;Cmax=1.08±0.19 ng/ml;AUC=173.46±114.66 ng/ml·h-1.The relative bioavailability of the domestic suspension was 90.5%.Conclusion No significant pharmacokinetic difference has been found between the domestic and the imported astemizole suspensions.

关 键 词：阿斯咪唑 混悬剂 放射免疫法 药物代谢动力学 生物利用度 

分 类 号：R969.1[医药卫生—药理学]