摘要
目的评价国产溴莫普林胶囊与进口hyprim片的生物等效性 ,为其临床应用提供试验依据。方法采用单剂双交叉试验设计 ,以乙萘酚为内标 ,采用高效液相色谱法测定血中溴莫普林浓度 ,计算药代动力学参数及试验制剂的相对生物利用度 ,评价两制剂的生物等效性。结果溴莫普林试验制剂和参比制剂主要药代动力学参数t1/2(α) 分别为(2.1±1.0)和(1.9±0.9)h ,t1/2(β)分别为(43.2±4.8)和(42.4±4.3)h ,Tpeak 分别为(3.4±1.6)和(3.1±1.5)h ,Cmax 分别为(5.9±0.9)和(5.9±1.0)μg·ml-1,AUC0～132 分别为(360.2±55.3)和(358.7±52.6)μg·h·ml-1,AUC0～∞ 分别为(423.8±56.0)和(422.5±51.1)μg·h·ml-1。试验制剂溴莫普林胶囊相对生物利用度F为(99.7±4.8) %。结论溴莫普林试验制剂和参比制剂单剂口服双交叉试验AUC0～132 无显著性差异(P>0.05)。进一步双单侧t检验和(1～2α)置信区间分析个体间、周期间和剂型间符合生物等效的假设 。
Aim To evaluate the bioequivalence of demestic brodimoprim capsules and imported hyprim tablets and provide experimental basis for clinical application.Methods A single dosage of Brodimoprim or hyprim was given to 18 healthy volunteers in a randomized 2_way cross_over test and the brodimoprim concentrations in plasma were determined by HPLC with β_naphtol as internal standard.The pharmacokinetic parameters and the relative bioavailability of the two preparations were calculated and their bioequivalence was evaluated.Results The major pharmacokinetic parameters of test and reference preparations were as follows respectively:t1/2(α)(2.1±1.0) and (1.9±0.9) h,t1/2(β)(43.2±4.8) and (42.4±4.3) h,Tpeak(3.4±1.6) and (3.1±1.5) h,Cmax(5.9±0.9) and (5.9±1.0)μg·ml-1,AUC0～132(360.2±55.3) and (358.7±52.6) μg·h·ml-1,AUC0～∞(423.8±56.0) and (422.5±51.1) μg·h·ml-1. The relative bioavailability (F) of brodimprim capsules was (99.7±4.8)%?Conclusion The multi_factorial analysis of variance showed that there was no significant difference in AUC0～132 between the test and reference preparations (P>0.05).The bioequivalent assumption was proved by further two one_side t_test and (1～2 α) confidence interval analysis in individuals,periods and forms of these two preparations.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2001年第1期53-55,共3页
Chinese Journal of Clinical Pharmacology and Therapeutics
