硝苯地平骨架控释片的制备及其体外释放性能

Preparation and in vitro Release Property of Nifedipine Matrix Tablet

研制了硝苯地平口服骨架控释片,考察了片剂处方和主要制备参数对药物释放速率的影响。通过对硝苯地平口服骨架片的制备工艺和处方组成进行优化,确定最优片剂处方为:硝苯地平固体分散体(硝苯地平与羟丙基甲基纤维素质量比为1∶1)60mg,聚环氧乙烷20mg,甘露醇10mg;采用粉末直接压片方法,压制硬度为(85±10)N的硝苯地平控释骨架片。体外释放研究表明,在14h内药物的释放度为89.69%,释放曲线的线性相关度为0.9962,具有良好的零级释放特性。这为研制恒速释放的硝苯地平制剂提供了一种新思路。

Hydrophilic matrix tablets of nifedipine（NFP） were prepared, together with the examination of the influences of formulation and preparation parameters on the drug release profiles. The optimal formulation obtained was ： nifedipine solid dispersion [ m （NFP） ：m （HPMC） = 1 ： 1 ） 60 mg, PEO 20 mg and mannitol 10 mg. The mixture was compressed directly and the hardness of the tablet was （85 ± 10） N. The cumulative release rate within 14h was 89.69%. Linear relationship between the accumulated release data and the time is 0. 996 2. It shows an excellent zero-order release profile in vitro for 14 h.