左甲状腺素钠2种制剂的人体生物等效性

Bioequivalence study of two kinds of levothyroxine sodium formula tablets in healthy Chinese subjects

目的:研究左甲状腺素钠片Berlthyrox(50μg(受试制剂)和雷替斯(50μg(参比制剂)的人体生物等效性。方法:按照两制剂两周期随机交叉设计,26名男女健康受试者单剂量口服(50μg/片×12片)或参比制剂(50μg/片×12片)。采用放射免疫法测定血清中甲状腺素(T4)、三碘甲腺原氨酸(T3)浓度。结果:Berlthyrox(50μg和雷替斯(50μg T4的主要药动学数据为AUC0-48h(5 682.6±828.7)和(5 746.8±776.1)μg.L-1.h,Cmax(141.2±22.3)和(148.5±21.7)μg.L-1t、max(2.6±1.1)和(2.3±1.2)h,T3的主要药动学数据为AUC0-48h(61.2±8.9)和(62.8±9.5)μg.L-1.h、Cmax(1.44±0.22)和(1.50±0.24)μg.L-1t、max(35.8±19.6)和(38.9±16.3)h;Berlthyrox(50μg对雷替斯(50μg T4、T3的相对生物利用度分别为(99.2±9.8)%、(97.9±9.0)%。结论:Berlthyrox(50μg和雷替斯(50μg生物等效。

OBJECtIVE To evaluate the relative bioavailibility and bioequivalence of new and old imported levothyroxine so- dium tablets Berlthyrox 50μg and Letrox 50μg in Chinese healthy subjects. METHODS 26 subjects （13 female, 13 male） were orally given with 600 μg （12 tablets） of different preparation forms in an open randomized cross 2 over test. The serum concentrations of total T4 and T3 were detected by radioimmunoassay. RESULTS The pharmacokinetic parameters for T, of Berlthyrox 50 μg were as follows： （5 682. 6± 828. 7） and （5 746. 8 ± 776. 1） μg·L^-1 .h for AUG0-48h, （141.2 ± 22. 3） and （148. 5 ± 21.7） μg. L^-1 for Cmax, （2. 6 ± 1.1 ） and （2. 3 ± 1.2） h for tmax. The pharmacokinetic parameters for T3 of Berlthy- rox 50μg were as follows： （61.2 ± 8. 9） and （62. 8 ＋- 9. 5）μg·L^- 1·h for AUG,48 h, （1. 44± 0. 22） and （1.50 ± 0.24） μg.L^- 1 for Cmax, （35.8 ± 19. 6） and （38. 9 ± 16. 3） h for tmax, respectively. The relative bioavailability for T4 of Berlthyrox 50 μg was （99. 2± 9. 8） %. The relative bioavailability for T3 of Berlthyrox 50 μg was （97.9 ± 9. 0） %. CONCLUSION Berlthyrox 50 μg and Letrox 50 μg are bioequivalent.