【摘要】 目的 :选择 12名男性健康志愿者 ,进行单剂量口服茶碱缓释胶囊的人体生物等效性评价。方法 :采用反相高效液相色谱法 ,以紫外 2 73nm为检测波长 ,测定了单剂量口服 2 0 0mg国产茶碱缓释胶囊受试药品在健康人体内的茶碱浓度 ,并与进口茶碱缓释胶囊参比药品进行对照。结果 :茶碱缓释胶囊的体内动态过程呈一级吸收的一房室开放模型 ,国产受试药品和进口参比药品的Cmax分别为 ( 5 12± 0 74 )mg/L和 ( 5 14±0 63 )mg/L ,tmax分别为 ( 5 4± 1 0 )h和 ( 5 3± 1 1)h ,MRT分别为 ( 17 79± 1 4 8)h和 ( 17 61± 1 78)h ,t1/ 2分别为 ( 10 55± 0 75)h和 ( 10 59± 1 10 )h ,AUC0 - 36 分别为 ( 85 3 3± 10 56)mg·h/L和( 86 2 6± 8 80 )mg·h/L。结论 :以体内茶碱AUC0 - 36 数值表征的国产茶碱缓释胶囊的相对生物利用度为( 98 9± 6 4 ) % ;选择Cmax、AUC0 - 36 和AUC0 -∞ 进行三因素方差分析与双单侧t检验 ,结果表明国产茶碱缓释胶囊和进口茶碱缓释胶囊两种制剂具有生物等效性。更多还原

【Abstract】 OBJECTIVE:To evaluate the bioequivalence assessment of theophylline sustained release capsules in healthy volunteers.METHODS:A reversed phase high performance liquid chromatography (RP HPLC) method was established for the determination of theophylline in plasma after a single oral dose of 200mg domestic theophylline sustained release capsules and imported theophylline sustained release capsules in a randomized crossover design. The detector was operated at UV 273nm.RESULTS:The dynamic course of theophylline plasma concentrations conformed to a one compartment open model with a 3P87 program and the main pharmacokinetic parameters after a single oral dose of 200mg domestic sustained release capsules and imported sustained release capsules were as follows: C max were (5 12±0 74)mg/L and (5 14±0 63)mg/L, t max were (5 4±1 0)h and (5 3±1 1)h, MRT were (17 79±1 48)h and (17 61±1 78)h, t 1/2 were (10 55±0 75)h and (10 59±1 10)h, AUC 0-36 were (85 33±10 56)mg·h/L and (86 26±8 80)mg·h/L,respectively.CONCLUSIONS:The relative bioavailability of domestic theophylline sustained release capsules is (98 9±6 4)%.The results of statistical analysis for C max ,AUC 0-36 and AUC 0-∞ showed that domestic sustained release capsules and imported sustained release capsules were bioequivalent.更多还原