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目的评价单硝酸异山梨酯片在健康人体相对生物利用度及生物等效性。方法受试者随机、自身双交叉、单剂量口服受试制剂和参比制剂20mg,采用LC/MS法测定血浆中药物浓度,药动学参数采用DAS软件处理获得。结果两种制剂Cmax分别为(486.19±108.22)、(465.62±87.188)ng·ml-1,Tmax分别为(0.62±0.33)、(0.79±0.49)h,t1/2分别为(4.51±0.60)、(4.60±0.75)h,AUC0-tn分别为(3195.75±421.77)、(3222.92±386.83)ng·h·ml-1,AUC0-∞分别为(3350.90±452.63)、(3390.83±401.04)ng·h·ml-1;相对于参比制剂,受试制剂的生物利用度F0-tn为(99.96±13.25)%。受试制剂和参比制剂的Cmax、AUC0-tn和AUC0-∞经对数转换后进行方差分析,两制剂间无显著性差异(P>0.05)。结论两种单硝酸异山梨酯片均具有生物等效性。
Objective To evaluate the relative bioavailability and bioequivalence of isosorbide mononitrate tablets in healthy volunteers. Methods Subjects were randomized, double crossover, single dose oral test formulation and reference formulation 20mg. The drug concentration in plasma was determined by LC / MS. The pharmacokinetic parameters were obtained by DAS software. Results The Cmax of the two preparations were (486.19 ± 108.22) and (465.62 ± 87.188) ng · ml-1, respectively, and the Tmax were (0.62 ± 0.33) and (0.79 ± 0.49) , (4.60 ± 0.75) h and AUC0-tn were (3195.75 ± 421.77) and (3222.92 ± 386.83) ng · h · ml-1 respectively. The AUC0-∞ were 3350.90 ± 452.63 and 3390.83 ± 401.04 ng · h · ml-1; the bioavailability F0-tn of the test formulation was (99.96 ± 13.25)% relative to the reference formulation. The Cmax, AUC0-tn and AUC0-∞ of the tested and reference preparations were logarithmically transformed and analyzed by ANOVA. There was no significant difference between the two preparations (P> 0.05). Conclusions Both isosorbide mononitrate tablets are bioequivalent.