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目的对富马酸酮替芬分散片在健康人体中的药代动力学特征及其生物等效性进行分析和评价。方法选取健康自愿者24例为研究对象,进行双周期自身交叉试验,分别单剂服用富马酸酮替芬分散片(试验品)或者富马酸酮替芬片(比照品),对2种药物的药代动力学特征(t_(max)、C_(max)、t_(1/2)及AUC_((0~36 h)))进行分析,并掌握试验品的生物利用度。结果试验品的t_(max)、C_(max)、t_(1/2)及AUC_((0~36 h))分别是(2.8±1.3)h、(403±155)ng/L、(5.7±1.9)h、(2 861±1 030)ng·h~(-1)·L~(-1),比照品分别为(3.1±1.1)h、(391±148)ng/L、(5.8±2.1)h、(2 843±984)ng·h~(-1)·L~(-1),相比较差异有统计学意义(P<0.01);试验品的生物利用度为(113±41)%。结论富马酸酮替芬分散片具有较好的水溶性和生物利用度,口服吸收性较强,和富马酸酮替芬片的生物等效性一致。
Objective To analyze and evaluate the pharmacokinetics and bioequivalence of ketotifen fumarate dispersible tablets in healthy volunteers. Methods Twenty-four healthy volunteers were selected as subjects for the study. Two-cycle self-crossover trials were conducted. Ketotifen fumarate dispersible tablets (test samples) or ketotifen fumarate tablets (reference samples) Pharmacokinetic characteristics (t max, C max, t 1/2 and AUC 0-36 h) of the drug were analyzed and the bioavailability of the test substance was determined. Results The values of t max, C max, t 1/2 and AUC 0 ~ (h) were (2.8 ± 1.3) h, (403 ± 155) ng / L and (3.1 ± 1.1) h, (391 ± 148) ng / L, (5.8 ± 1.9) h and (2861 ± 1030) ng · h -1 · L -1 ± 2.1) h and (2 843 ± 984) ng · h -1 · L -1, respectively, with significant difference (P <0.01). The bioavailability of the test product was (113 ± 41)%. Conclusions Ketotifen fumarate dispersible tablets have better water solubility and bioavailability, have stronger oral absorption and are consistent with the bioequivalence of ketotifen fumarate tablets.