单硝酸异山梨酯阿司匹林缓释片在人体内的药动学及生物等效性

20名健康受试者随机交叉单剂量(单硝酸异山梨酯60mg和阿司匹林75mg)和多剂量口服单硝酸异山梨酯阿司匹林缓释片(受试制剂)、单硝酸异山梨酯缓释片及阿司匹林肠溶片(参比制剂)后,分别采用HPLC-MS法和HPLC-UV法测定人血浆中单硝酸异山梨酯和水杨酸浓度。药动学参数见文中表1和表2。经双单侧t检验结果表明,以单硝酸异山梨酯为研究对象,两制剂具有生物等效性;以阿司匹林为研究对象,两制剂的吸收程度相当,但受试制剂吸收速度较快。

Pharmacokinetics and Bioequivalence of Isosorbide Mononitrate and Aspirin Sustained-Release Tablets in Human

According to a randomized crossover design,the pharmacokinetics and bioequivalence after single or multiple dose oral administration of isosorbide mononitrate/aspirin sustained-release tablets (test preparations), isosorbide mononitrate sustained-release tablets and aspirin enteric-coated tablets (reference preparations) in 20 healthy male volunteers were investigated.The concentrations of isosorbide mononitrate and salicylic acid in plasma were determined by HPLC-MS and HPLC-UV,respectively.The main pharmacokinetic parameters were showed in Tab1 and Tab2.The test preparation showed bioequivalence for the isosorbide mononitrate component with isosorbide mononitrate sustained-release tablets,and equivalent AUC for the aspirin component with aspirin enteric-coated tablets,but the test preparation was more rapidly absorbed for the aspirin component than the reference preparation.