富马酸比索洛尔分散片人体药动学与生物等效性研究  

Pharmacokinetics and Bioequivalance of Bisoprolol Hemifumarate Dispersed Tablet in Healthy Volunteers

作　　者：蔡军[1] 徐文炜[1] 张红[1] 胡晓[1] 程晓华[1] 温金华[1] 熊玉卿[1] 

机构地区：[1]南昌大学医学院临床药理研究所,330006

出　　处：《医药导报》2008年第3期271-274,共4页Herald of Medicine

摘　　要：目的研究富马酸比索洛尔分散片在健康人体内的药动学,评价两种制剂的生物等效性。方法采用随机自身交叉双周期设计方法,将20例健康男性受试者随机分为两组各10例,分别单次交叉口服等剂量比索洛尔供试制剂或参比制剂10 mg,采用高效液相色谱-荧光检测法测定血浆中比索洛尔的浓度,计算其药动学参数和相对生物利用度,评价两制剂的生物等效性。结果供试制剂和参比制剂比索洛尔实测AUC0-48 h分别为（628.04±136.61）和（641.24±161.20）ng·h·mL^-1,Cm ax分别为（46.78±12.03）和（47.91±12.74）ng·mL^-1,tm ax分别为（2.4±0.8）和（2.1±0.8）h,t1/2分别为（9.97±1.70）和（9.71±1.23）h。供试制剂相对于参比制剂的生物利用度为（103.1±30.8）%。结论比索洛尔供试制剂和参比制剂具有生物等效性。Objective To investigate pharmacokinetic and bioequivalance of bisoprolol hemifumarate dispersed tablet in healthy volunteers. Methods Twenty volunteers were randomly divided into 2 groups. A single oral dose of 10 mg of test or reference tablets was delivered to each volunteer in an open crossover test. The plasma concentration of bisoprolol hemifumarate was determined by HPLC fluorescence detection. Based on the parameters of pharmacokintic and relative bioavailability, the bioequivalance of bisoprolol hemifumarate was evaluated. Results AUC0-48 h in 2 groups was （628. 04±136. 61） and （641.24±161.20） ng·h·mL^-1 respectivly; Cmas was 46.78±12.03） and （47.91±12.74） ng·mL^-1 in 2 groups; tmax was （2.4±0.8h） and （2.1±0.8）h; t1/2 was （9.97±1.70 ） and （9.71±1.23） h in 2 groups. The relative bioavailability of bisoprolol hemifumarate dispersed tablet was （103.1±30.8）%. Conclusion The two preparations of bisoprolol hemifumarate dispersed tablet and reference tablets are bioequivalent.

关 键 词：比索洛尔 富马酸 药动学 生物等效性 色谱法 高压液相 

分 类 号：R972.4[医药卫生—药品] R969[医药卫生—药学]