左甲状腺素钠2种配方片剂人体生物利用度比较  

Bioavailibility of two kinds of levothyroxine sodium formula tablets in healthy subjects

作　　者：荣征星[1] 赵咏桔[2] 陈广洁 王昊[1] 席晔斌 张颖德 陆洁莉[2] 刘玥[2] 姜昌斌[2] 陈红专[1] 

机构地区：[1]上海第二医科大学药理学教研室,上海200025 [2]瑞金医院国家药品临床研究基地,上海200025 [3]上海市免疫研究所,上海200025

出　　处：《中国新药与临床杂志》2005年第1期7-10,共4页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的:评价进口新配方与旧配方左甲状腺素钠片剂的人体相对生物利用度及生物等效性。方法:24名健康男性受试者,随机分为2组,分别于早晨空腹单剂量口服新配方或旧配方左甲状腺素钠片600μg。35d清洗期后再交叉给药。分别在服药前30,15,4min内和服药后0.5,1.0,1.5,2.0,2.53.0,3.5,4.0,6.0,8.0,10.0,12.0,18.0,24.048.0h取静脉血,用放射免疫分析法测定血清样品T4和T3的浓度。结果:受试者口服新配方和旧配方左甲状腺素钠片剂后血清中T4呈明显时量变化主要药动学参数如下:tmax为(3.4±s2.3)和(3.5±2.1)h,cmax为(168±39)和(160±34)μg·L-1AUC0～48为(5640±1060)和(5620±1010)μg··L-1。而血清中T3无明显时量变化。结论:新配方和旧配方左甲状腺素钠片剂相对生物利用度为(102±18)%,2种配方的制剂具有生物等效性。AIM: To evaluate the relative bioavailibility and bioequivalence of new and old imported levothyroxine sodium tablets in Chinese healthy sub-jects. METHODS: The study was performed in 24 healthy male volunteers according to a randomized 2-way crossover design with a washout period of 35 d. The blood samples were collected at 30,15,<4 min before and 0.5, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 6.0, 8.0, 10.0, 12.0, 18.0, 24.0, 48.0 h after taking 600 μg of two kinds of levothyroxine sodium tablets. The concentrations of serum total T 4 and T 3 were determined by radioimmunoassay. RESULTS: The serum T 4 concentration showed obvious changes with time following administration of two kinds of tablets.The pharmacokinetic parameters for the new and old tablets were as follows:(3.4±s 2.3) and (3.5± 2.1) h for t max, (168±39) and (160±34) μg·L -1 for c max, (5 640±1 060)and (5 620± 1 010) μg·h·L -1 for AUC 0-48, respectively. However, the serum T 3 concentration did not change significantly after administration of both kinds of tablets. CONCLUSION: The relative bioavailability of new levothyroxine sodium tablet is (102±18) %. The new and old levothyroxine sodium tablets are bioequivalent.

关 键 词：甲状腺素 片剂 生物利用度 药物稳定 性 放射免疫测定 左甲状腺素钠 处方 

分 类 号：R977.14[医药卫生—药品] R969.1[医药卫生—药学]