灯盏花素分散片人体生物等效性研究  

Bioequivalence Study of Breviscapine Dispersible Tablets in Chinese Healthy Volunteers

作　　者：贾云[1] 张军[2] 储继红[2] 谈恒山[2] 蒋萌[2] 熊宁宁[2] 居文政[2] 

机构地区：[1]扬子江药业集团有限公司,泰州225321 [2]南京中医药大学附属医院临床药理科,南京210029

出　　处：《药学与临床研究》2010年第4期347-349,共3页Pharmaceutical and Clinical Research

基　　金：江苏省中医药领军人才项目(2009)

摘　　要：目的：以灯盏花素普通片为对照,研究灯盏花素分散片在健康人体内的相对生物利用度和生物等效性。方法：20名健康成年男性志愿者采用随机分组、自身交叉对照试验设计,用LC-MS法测定血浆中灯盏乙素苷元,线性范围为0.013~3.32μg.mL-1;平均回收率89.7%-100.5%,日内和日间精密度均小于12.0%。结果：灯盏花素分散片和普通片的主要药动学参数：tmax：（7.1±2.2）h和（6.6±1.9）h;Cmax：（0.87±0.37）mg.L-1和（1.0±0.44）mg.L-1;AUC（0-24h）：（4.68±1.53）mg·h·L^-1和（5.08±1.50）mg·h·L^-1;AUC（0-∞）：（4.78±1.55）mg·h·L^-1和（5.18±1.54）mg·h·L^-1.h;t1/2：（4.36±2.07）h和（4.09±1.35）h。以AUC（0-24h）计算的受试制剂的相对生物利用度为（93.1±16.9）%。结论：两种制剂的Cmax和AUC（0-24h）经方差分析和双单侧t检验其结果生物等效。Objective：To evaluate the relative bioavailability and bioequivalence of breviscapine dispersible tablets（test） to the normal tablets（reference） in Chinese healthy volunteers.Methods：Twenty male healthy volunteers were randomized to receive a single crossover oral dose of 120mg breviscapine tablets or dispersible tablets.The plasma concentration of scutellarin aglycone was determined by an LC-MS method with the linear range at 0.013-3.32μg.mL^-1 and inter-and intra-day RSD less than 12%.The bioequivalence was analyzed using BAPP2.2 program.Results：The main pharmacokinetic parameters showed without significant differences between the tablets test vs.reference,and they were as follows：tmax：（7.1±2.2） vs.（6.6±1.9）h,Cmax：（0.87±0.37） vs.（1.0±0.44）mg.L^-1,AUC（0-24h）：（4.68±1.53） vs.（5.08±1.50） mg.L^-1.h,AUC（0-∞）：（4.78±1.55） vs.（5.18±1.54） mg.L^-1.h,t1/2：（4.36±2.07） vs.（4.09±1.35）h,F0-24h was（93.1 ±16.9）%.The results of variance analysis and two-one sided t-test showed that there was no significant difference between the two formulations in the AUC or Cmax.Conclusion：The breviscapine dispersible tablets were bioequivalent to the reference tablets.

关 键 词：灯盏花素分散片 高效液相-质谱联用法 药代动力学 生物等效性 

分 类 号：R969.1[医药卫生—药理学]