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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。
OBJECTIVE: To evaluate the relative bioavailability and bioequivalence of imported new prescription and the old prescription of levothyroxine sodium tablets. Methods: Twenty-four healthy male subjects were randomly divided into two groups. One hundred and sixty μg of levothyroxine sodium tablets were orally administered in the morning fasting single dose. After 35d cleaning period and then cross-administered. Venous blood was taken within 30,15,4 minutes and 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 before taking the drug and radioimmunoassay Method for the determination of serum samples T4 and T3 concentrations. Results: The main pharmacokinetic parameters of T4 in the serum of the new formula and the old prescription levothyroxine sodium tablets were as follows: tmax was (3.4 ± s2.3) and (3.5 ± 2.1) h, The values of cmax were (168 ± 39) and (160 ± 34) μg · L-1AUC0 ~ 48, which were 5640 ± 1060 and 5620 ± 1010 μg ··L-1, respectively. Serum T3 no significant change in time. CONCLUSION: The relative bioavailability of the new formulation and the old formulation of levothyroxine sodium tablets is (102 ± 18)%. The formulations of the two formulations are bioequivalent.