马来酸罗格列酮胃漂浮型缓释片的研究

Studies on Rosiglitazone Maleate Intragastric Floating Sustained Release Tablet

目的 根据流体动力学平衡控释原理 (HBS)研制了马来酸罗格列酮胃漂浮型缓释片。方法 以体外释放度和漂浮情况为筛选指标 ,采用单因素考察和正交试验设计相结合 ,对胃漂浮缓释片的处方、制备工艺及体外释放条件进行优化筛选 ;采用γ闪烁照相技术对优化处方的体内漂浮情况进行胃内动态观察 ;结果 马来酸罗格列酮胃漂浮缓释片在释放介质中迅速起漂 ,持漂时间超过 12h ,12h达最大累积释放 ;初步确定在胃内滞留时间达 3h以上 ;结论 优化处方的释放过程符合Higuchi方程 ,释放机制为异常扩散 ;

AIM Rosiglitazone maleate intragastric floating sustained release tablet was developed based on the hydrodynamically balanced drug delivery system, which could prolong the residence time of drug in the stomach and improve the bioavailability. METHODS The amount of expicents, preparing methods and drug release \%in vitro\% of the formulation were determined by floating and drug releasing conditions as screening index with orthogonal design test and single factor test methods. Rosiglitazone maleate sustained release tablet and traditional tablet (Avandia) were radio labeled with 99 mTc, and their behavior in stomach was detected by r ray camera techniques. RESULTS\ The optimum formulation kept sustained floating and release in media for 12 h. The floating tablet was remained in the stomach for more than 3 h without disintegrating. CONCLUSION\ Drug release of sustained release tablet in media was in agreement with Higuchi equation, and the releasing mechanism was irregular diffusion. The gastric residence time of the subjects after oral administration floating tablet was obviously longer than that after oral administration conventional tablet.