富马酸异丙吡仑片的人体生物等效性

Study of the bioequivalence of isopropiram fumarate tablets in healthy volunteers

目的：研究富马酸异丙吡仑片的人体相对生物利用度。方法：健康志愿者20名。随机双交叉单剂量口服富马酸异丙吡仑试验和参比制剂，用高效液相色谱法测定血浆中异丙吡仑的浓度。用3p97药动学程序计算相对生物利用度和评价生物等效性。AUC0.36，AUC0-inf和Cmax方差分析和双单侧t检验，tmax进行秩和检验。结果：单剂量口服试验制剂和参比制剂后血浆中的异丙吡仑的Cmax分别为（1．10±0．14）mg·L^-1和（1、09±0．15）mg·L^-1；tmax分别为（1．8±0.5）h和（1、9±0．6）h；AUC0.36分别为（9．1±1．9）mg·h·L^-1和（9．2±2．3）mg·h·L^-1；AUC0-inf分别为（9.6±2.0）mig·h·L^-1和（9．9±2．4）mg·h·L^-1；Cmax,AUC0—36、AUC0-inf的90％可信区间分别为94．6％-107．1％、92.1％-106.1％、90．0％-106．2％。结论：试验制剂与参比制剂的人体相对生物利用度为（100．4±17．8）％，试验制剂和参比制剂具有生物等效性。

OBJECTIVE To study the relative bioavailability of isopropiram fumurate tablets in healthy volunteers. METHODS A single oral dose （200 mg of test and reference formulation） were given to 20 healthy volunteers in a randomised crossover study. The concentrations of Isopropiram in plasma were determined by HPLC. The pharmaeokineties parameters were calculated and the bio- availability and bioequivalenee of two formulations were evaluated by 3p97 program. RESULTS After a single dose, the pharmacokineties parameters for Isopropiram were as follows： Cmax were （ 1.10 ± 0.14 ） mg· L^ - 1 and （ 1.09 ± 0.15 ） mg·L ^- 1 ; tmax were （ 1.8 ± 0.5 ） h and （1.9±0.6）h; AUC0.36 were （9.1±1.9）mg·h·L^-1 and （9.2±2.3） mg·h·L^-1 ;AUC0.inf were （9.6 ±2.0）mg·h·L^-1 and （ 9.9± 2.4） mg· h· L^-1 for T and R respectively. The 90% confidential interval of Cmax,AUC0.36 and AUC0-inf Of tested formulation were 94.6% - 107.1% ,92.1% - 106.1% and 90.0% - 106.2% respectively. CONCLUTION The relative bioavailability is （ 100.4 ± 17.8 ）% ; The results of the statistic analysis show that the two formulations are bioequivalent.