吲达帕胺缓释片的研制及释药机理考察

Development of indapamide sustained release tablets and study on its release mechanism

目的 :研制吲达帕胺缓释片 ,并考察其释药机理。方法 :以HPMC为骨架材料 ,以微晶纤维素、乳糖和可压性淀粉调节释放度 ,对吲达帕胺缓释片的影响因素进行了考察 ,并采用正交试验设计筛选处方。结果 :吲达帕胺缓释片的组成为 :HPMCK4M 3 7.5mg,HPMCK15M 7.5mg,乳糖 45 .0mg,可压性淀粉 3 7.5mg,微晶纤维素 2 1.0mg,硬脂酸镁 1.5mg,药物的释放符合零级动力学方程 ,释放机制为骨架溶蚀机制 ;释药速率受介质 pH值的影响 ,几乎不受压片压力的影响。 结论 :研制的吲达帕胺缓释片体外释放符合国外同类产品的释药特性。

OBJECTIVE To develop indapamide sustained release tablets and study the release mechanism. METHODS The effects on the release of indapamide sustained release tablets were observed, and the formulations were screened by the use of HPMC as the gel matrix and MCC, Lactose and Starch to modify the release and by the method of Orthogonal Test. RESULTS The excipient composition of indapamide sustained release tablet is:HPMC K4M 37.5 mg , HPMC K15M 7.5 mg , Lactose 45.0 mg , Starch 37.5 mg , MCC 21.0 mg ,Magnesium stearate 1.5 mg .The release behavior of the tablets followed with the zero order kinetic equation, and it was properly characterized by the erosion mechanism, influenced by pH of the media, without the influence of the tablet hardness. CONCLUSIONS The selected formulation of Indapamide sustained release tablets have the same drug release characteristics as the import product NATRILIX SR.