硝苯地平缓释片体内外相关性研究

In Vivo and in Vitro Correlation Study of Nifedipine Sustained Release Tablets

目的:采用反卷积法进行硝苯地平缓释片体内外相关性的研究。方法:建立硝苯地平缓释片的体外溶出方法,并绘制其体外溶出曲线。然后以硝苯地平静脉注射的人体内血药浓度为权函数,采用反卷积法计算体内释药特性,再与相应的体外溶出曲线进行比较,考察硝苯地平缓释片的体内外相关性。结果:硝苯地平缓释片体外溶出结果较理想,但体内外相关性较差。结论:浆法不能较准确地模拟硝苯地平缓释片在体内的释放行为,体外溶出方法有待进一步研究。

Objective:To evaluate the in vitro/in vivo correlation for nifedipine sustained release tablets using deconvolution method.Methods:To establish an in vitro dissolution method for nifedipine sustained release tablets,and to draw the dissolution curve.The percentage of absorption was calculated by deconvolution method using data of plasma concentration from nifedipine sustained release tablets,which the in vivo data of nifedipine sustained release tablets after oral administration was used as weight function.It was compared with data of in vitro release to assess the in vitro/in vivo correlations.Results:The dissolution of nifedipine sustained release tablets was satisfactory in vitro,but the correlation between in vivo and in vitro was poor.Conclusions:The release behavior of nifedipine sustained-release tablets in vivo can not be accurately simulated by slurry method,and the dissolution method in vitro needs further study.