奥美拉唑肠溶胶囊人体药代动力学和相对生物利用度研究  

Study of omeprazole enteric-coated capsules on its pharmacokinetics and relative bioavailability in man

作　　者：代宗顺[1] 汪敏燕 顾世芬[1] 杨德隆[1] 曾繁典[1] 

机构地区：[1]同济医科大学临床药理室,武汉430000 [2]浙江金华康恩贝生物制药有限公司,金华321016

出　　处：《中国现代应用药学》2002年第2期125-128,共4页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的 :研究奥美拉唑肠溶胶囊在健康人体内的药代动力学和相对生物利用度。方法 :采用 HPL C法测定 8名男性健康志愿受试者随机交叉一次口服康恩贝产 (受试品 ,商品名金奥康 )和瑞典产 (参比品 ,商品名洛赛克 )奥美拉唑胶囊各 40 mg的血药浓度 ,进行人体生物利用度研究。结果 :两种胶囊的药—时曲线和药代动力学特征均符合—室开放模型。测得主要药代动力学参数为 :试验胶囊和参比胶囊从胃肠吸收的滞后的时间 (L.T)分别为 1.3 6± 0 .92 h和 0 .90± 0 .42 h;Cmax分别为 0 .2 8±0 .2 0 mg/L 和 0 .3± 0 .2 0 mg/L;;Tmax分别为 3 .69± 1.46h和 2 .44± 0 .74h;AUC分别为 1.71± 1.2 0 mg/L· h和 2 .44±0 .74mg/L· h;消除半衰期分别为 2 .3 4± 0 .61h和 2 .2 2± 0 .70 h;结论 :奥美拉唑试验胶囊的相对生物利用度为 10 2 .5± 16.1%。OBJECTIVE:To study the pharmacokinetics and relative bioavailability of omeprazole enteric coated capsules in healthy subjects.METHOD:A randomie controlled self crossed study was carried out. 40mg of the test drug Kin kong and the control drug Losec were given to 8 male healthy volunteers. Plasma concentrations were measured by HPLC.RESULTS:It was found that the two capsules obeyed one compartment open model. The main pharmacokinetic parameters were:the lag time (T lag )of test drug and control drug were 1.36±0.92h and 0.90±0.42h, respectively after gastrointestinal tract absorption, the mean peak plasma concentrations (C max ) were 0.28±0.20mg/L and 0.3±0.20mg/L respectively,the mean time (T max ) were 3.69±1.46h and 2.22±0.74h respectively, the area under the curve (AUC) were 1.71±1.20mg/L·h and 2.44±0.74mg/L/h respectively, and the half clearance time (T 1/2β ) were 2.34±0.61h and 2.22±0.70h respectively. The relative bioavailability of Kin kong was 102.5±16.1%. There was no statistical significant difference between CONBA product and Sweden product on bioequivalent.

关 键 词：奥美拉唑 高效液相色谱 生物利用度 药代动力学 研究 抗溃疡药 

分 类 号：R975.6[医药卫生—药品] R944.5[医药卫生—药学]