摘要
目的考察格列吡嗪控释片体外药物释放特征和体内外相关性。方法分别采用3种不同pH值的缓冲溶液作为释放介质,并对pH6.8的释放介质分别采用3种不同的转速来测定格列吡嗪控释片的体外药物释放度,考察释放介质pH值和转速对释放度的影响。用Loo-Riegelman法计算格列吡嗪控释片在健康男性受试者体内吸收百分数,并与相应时间体外累积释放度线性回归,进行体内外相关性考察。结果格列吡嗪控释片在不同pH值释放介质中的释放度一致,均符合零级动力学,且不受转速影响。将体内累积吸收百分数y与相应时间在pH6.8释放介质中的体外释放百分数x进行线性回归(n=7),回归方程为y=0.6904x+22.941,r=0.9528。结论格列吡嗪控释片的释放度不受释放介质pH值和转速的影响,释药恒速。体外释放累积百分数与体内吸收百分数呈A级相关,具有良好的体内外相关性。
Objective To study the drug release characteristics in vitro and the correlation between the dissolution in vitro and the absorption in vivo of glipizide controlled-release tablets. Methods Three kinds of release media with various pH values were used respectively to study the effect of pH value on the drug release characteristic of glipizide controlled-release tablets. And for the release media of pH 6. 8, three rotating speeds were taken to study the effect on the drug release. The in vivo absorption per- cents in healthy male volunteers were calculated by Loo-Riegelman method. The correlation between the dissolution in vitro and the absorption in vivo was studied. Results The drug release profiles in different media with various pH values were similar. The drug release was not affected by the rotating speed within the range studied. The linear regressive equation established between the absorption percent in vivo and the dissolution percent in vitro of glipizide controlled-release tablets was y = 0. 690 4x ＋ 22. 941, r = 0. 952 8. Conclusion The pH value of release media and the rotating speed had no effect on the drug release. The drug release in vitro was of zero-grade dynamics. There was a significant correlation between the absorption in vivo and the drug release in vitro of glipizide controlled-release tablets.
出处
《国际药学研究杂志》
CAS
2009年第6期443-446,共4页
Journal of International Pharmaceutical Research
关键词
格列吡嗪控释片
药物释放
体内外相关性
glipizide controlled-release tablets
drug release
in vitro and in vivo correlation
