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目的了解富马酸酮替芬散片在健康人体内的药代动力学特征及其生物等效性。方法在2014年6月选取志愿受试者共计20名,采用双周期自身交叉试验设计法,分别口服2mg富马酸酮替芬片(参比品)或单剂量富马酸酮替芬散片(受试品)。观察并对比富马酸酮替芬分散片和富马酸酮替芬片的主要药动力学参数(tmax,cmax,t1/2及AUC(0~36)),观察富马酸酮替芬分散片的相对生物利用度。结果富马酸酮替芬分散片tmax,cmax,t1/2及AUC(0~36)分别为(2.9±1.2)h、(402±156)ng·L-1、(5.6±2.1)h、(2863±1032)ng/(h·L),富马酸酮替芬片tmax,cmax,t1/2及AUC(0~36)分别为(3.3±1.3)h、(392±149)ng·L-1、(5.7±2.3)h、(2794±973)ng/(h·L)。两者在人体药代动力学参数上进行比较,差异不具有统计学意义(P>0.05)。富马酸酮替芬分散片的相对生物利用度为(112±42)%。结论富马酸酮替芬分散片有较强的水溶性以及较高的生物利用度,且便于服用和吸收。富马酸酮替芬分散片与富马酸酮替芬片有相同生物等效性。
Objective To investigate the pharmacokinetics and bioequivalence of ketotifen fumarate tablets in healthy volunteers. Methods A total of 20 volunteers were selected in June 2014. Two-cycle self-crossover trial design was adopted. Oral administration of 2 mg ketotifen fumarate tablets (reference substance) or single dose ketotifen fumarate tablets (Test article). The main pharmacokinetic parameters (tmax, cmax, t1 / 2 and AUC (0 ~ 36)) of ketotifen fumarate dispersible tablets and ketotifen fumarate tablets were observed and compared. The effects of ketotifen fumarate dispersibility The relative bioavailability of the tablets. Results The tmax, cmax, t1 / 2 and AUC values of ketotifen fumarate dispersible tablets were (2.9 ± 1.2) h, (402 ± 156) ng · L-1 and (5.6 ± 2.1) (2863 ± 1032) ng / (h · L), and the tmax, cmax, t1 / 2 and AUC values of ketotifen fumarate were (3.3 ± 1.3) h and (392 ± 149) ng · L-1, (5.7 ± 2.3) h and (2794 ± 973) ng / (h · L), respectively. The two in the human pharmacokinetic parameters were compared, the difference was not statistically significant (P> 0.05). The relative bioavailability of ketotifen fumarate dispersible tablets was (112 ± 42)%. Conclusions Ketotifen fumarate dispersible tablets have strong water solubility and high bioavailability, and are easy to take and absorb. Ketotifen fumarate dispersible tablets and ketotifen fumarate tablets have the same bioequivalence.