单硝酸异山梨酯择时释放渗透泵片在家兔体内的药动学研究

Pharmacokinetics Study of Timed- and Controlled-Release Osmotic Pump System of Isosorbide Mononitrate in Rabbits

目的:考察单硝酸异山梨酯择时释放渗透泵控释片在家兔体内的药动学。方法:采用双周期交叉试验设计对所制备的单硝酸异山梨酯择时微孔渗透泵片和市售缓释片进行了家兔体内药动学考察。结果:两制剂Tmax分别为9.67 ± 0.31 h和2.68 ± 0.34 h,Cmax分别为178.23 ± 17.22 ng/ml和323.67 ± 35.75 ng/ml,MRT分别为12.25 ± 0.66 h和7.58 ± 0.80 h。结论:表明所制备的单硝酸异山梨酯择时释放渗透泵控释片的血药浓度较为平稳,时滞约4 h,能够较好的符合心血管疾病的发病规律。

Objective: To study the pharmacokinetics of isosorbide mononitrate timing microporous osmotic pump tablets in rabbits. Methods: Pharmacokinetics of isosorbide mononitrate timing microporous osmotic pump tablets and marked sustained release tablets were evaluated in rabbits through two period cross-over design. Results: The pharmacokinetic parameters of the test and reference formulation are as below: Tmax 9.67 ± 0.31 and 2.68 ± 0.34 h;Cmax 178.23 ± 17.22 and 323.67 ± 35.75 ng/ml;MRT 12.25 ± 0.66 and 7.58 ± 0.80 h, respectively. Conclusion: The results showed that the prepared isosorbide mononitrate timing microporous osmotic pump tablets with a lag time of about 4 h and a steady drug concentration, and it better complied with the circadian rhythms of cardiovascular diseases.