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目的:研究国产富马酸卢帕他定胶囊和普通片的人体生物等效性。方法:20名健康男性志愿者按2×2交叉试验方案设计,分别口服受试制剂和参比制剂各10mg,并采集24h内动态血标本;用HPLC/MS法测定血浆中卢帕他定浓度,计算药动学参数,并判定两种制剂的生物等效性。结果:受试制剂和参比制剂的主要药动学参数Cmax分别为(3.6±1.6)μg·L-1和(3.7±1.9)μg·L-1,tmax分别为(0.8±0.1)h和(0.8±0.1)h,AUC0-24分别为(12.3±7.1)μg·L-1.h和(13.1±9.5)μg·L-1.h,AUC0-∞分别为(13.1±7.5)μg·L-1.h和(13.9±10.0)μg·L-1.h,t1/2(ke)分别为(5.9±2.4)和(5.4±1.7)h,两制剂主要药动学参数经对数转换后进行方差分析及双单侧t检验,并计算90%置信区间,表明两种制剂生物等效,受试制剂的人体生物利用度为(100.4±19.3)%。结论:两种制剂生物等效。
Objective: To study the bioequivalence of domestic made rupatadine fumarate capsules and common tablets. Methods: Twenty healthy male volunteers were enrolled in a 2 × 2 crossover trial. Oral 10 mg of test and reference preparations were given orally and 24 h dynamic blood samples were collected. The plasma concentrations of rupatadine , Calculating pharmacokinetic parameters and determining the bioequivalence of the two formulations. Results: The main pharmacokinetic parameters Cmax were (3.6 ± 1.6) μg · L-1 and (3.7 ± 1.9) μg · L-1, respectively, and the tmax were (0.8 ± 0.1) h and (0.8 ± 0.1) h and AUC0-24 were (12.3 ± 7.1) μg · L-1.h and (13.1 ± 9.5) μg · L-1.h respectively, and AUC0-∞ were (13.1 ± 7.5) μg · L-1.h and (13.9 ± 10.0) μg · L-1.h, t1 / 2 (ke) were 5.9 ± 2.4 and 5.4 ± 1.7 h respectively. The main pharmacokinetic parameters of the two formulations were logarithmic After analysis, ANOVA and two-sided one-tailed t tests were performed. The 90% confidence interval was calculated, indicating that the bioavailability of the two preparations was 100.4 ± 19.3%. Conclusions: Both formulations are bioequivalent.