国产与进口盐酸依匹斯汀片人体药动学和相对生物利用度研究

目的:比较国产与进口盐酸依匹斯汀片在正常人体内的药动学与相对生物利用度。方法:18名健康志愿者随机交叉单剂量口服国产或进口盐酸依匹斯汀片20mg,采用高效液相色谱法测定血药浓度,用3p97软件包计算两者的药动学参数与相对生物利用度。结果:国产与进口片的药-时曲线符合口服吸收一房室摸型。tmax分别为(2.00±0.87)、(2.31±0.73)h,Cmax分别为(15.80±6.99)、(13.39±6.03)μg·L-1,AUC0~60分别为(185.36±68.07)、(191.69±71.31)μg·h·L-1,t1/2Ke分别为(10.90±4.06)、(12.64±4.66)h。国产片相对于进口片的生物利用度为(96.70±14.47)%,经配对t检验、方差分析、双单侧t检验及1~2α置信区间法统计分析,各药动学参数无显著性差异(P>0.05)。结论:国产片与进口盐酸依匹斯汀片生物等效。

Pharmacokinetics and Relative Bioavailability of Domestic versus Imported Epinastine Hydrochloride Tablets in Healthy Volunteers

OBJECTIVE： To study the pharmacokinetics and the relative bioavailabillty of domestic versus imported epinastine hydrochloride （EPST） tablets in healthy volunteers. METHODS： A single oral dose of 20 mg domestic EPST tablet or imported tablet was given to 18 healthy male volunteers in randomized crossover way. Plasma concentrations of tizanidine were measured by HPLC. The pharmacokinetic parameters as well as relative bioavailability were measured by 3p97 software. RESULTS： The concentration - time curves of both domestic EPST tablet and imported EPST tablet were in line with one - compartment open model, with tmax at （2.00±0.87） h and （2.31±0.73） h; Cmax（15.80±6.99） μg ·L^-1 and （13.93±6.03） μg· L^-1; AUC0- 60（185.36± 68.07）μg · h · L^-1 and （191.69± 71.31）μg · h · L^-1; t1/2Kε （10.90±4.06）h and （12.64± 4.66）h, respectively. The paired t - test, F - test, one- side and two - sided t - test and the 1-2 α confidence interval statistical analyses revealed that there were no significant differences between the two formulations in the tmax Cmax AUC0-60, t 1/2Kε （P 〉 0.05）. The relative bioavailability of domestic EPST tablets was （96.70± 14.47）%. CONCLUSION： The result of the statistical analysis showed that the two formulations of EPST were bioequivalent.