单硝酸异山梨酯片体内生物等效性研究

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。

Bioequivalence of Two Oral Formulations of Isosorbide Mononitrate Tablets in Healthy Volunteers

Aim To study the bioavailability and bioequivalence of the tested and reference isosorbide-5-mononitrate （IS-5-MN） tablets in healthy male volunteers. Methods According to the crossover design, each volunteer was orally given 20mg IS-5-MN. The plasma concentrations were determined by LC/MS. Pharmacokinetic parameters were obtained using DAS program. Results C max was（486. 19 ± 108.22） and （465.62 ± 87. 188 ） ng·ml^-1, T max was（0.62 ±0.33） and （0.79 ±0.49）h; t 1/2 was （4.51 ±0.60） and （4.60 ±0.75）h;AUC0-tn was （3 195.75 ± 421.77） and （3 222.92 ± 386.83 ） ng·h·ml^-1 and AUC0-∞ was （3 350.90 ± 452.63 ） and （3 390.83 ± 401.04） ng·h·ml^-1, respectively. The relative bioavailability was （99.96 ± 13.25 ）%. The data of the reference and tested drugs were not different as shown by F test. Conclusion The result shows that the two IS-5-MN tablets made in two different pharmacies are bioequivalent.