维格列汀三层缓释片的处方研究及体外释放行为表征

Formulation and in vitro release behavior of tri-layer vildagliptin sustained-release tablets

目的设计并制备维格列汀三层缓释片以期达到零级释放的效果,并考察其体外释放行为。方法采用羟丙基甲基纤维素(HPMC)作为凝胶型骨架缓释材料,利用三层压片技术制备维格列汀三层缓释片,采用零级释放方程以最小二乘法对制剂的体外释放数据进行拟合,以拟合方程的相关系数(r)为指标,采用单因素试验筛选维格列汀三层缓释片的含药层和阻滞层的处方组成。结果优化后的处方组成:上、下层为阻滞层,由HPMC K100M 200 mg、微晶纤维素198 mg、硬脂酸镁2 mg组成;内层为含药层,由维格列汀100 mg、HPMC K4M 50 mg、微晶纤维素48 mg、硬脂酸镁2 mg组成。维格列汀三层缓释片体外释放行为符合零级释药特征。结论成功制得具零级释放特征的维格列汀三层骨架缓释片。

Objective To prepare tri-layer vildagliptin sustained-release tablets aiming for zero-order release profile in vitro by the dissolution test.Methods Hydroxyl propyl methyl cellulose(HPMC)was used as the matrix material.The formulation of tri-layer vildagliptin sustained-release tablets was prepared by tri-layer tablets technique.According to the zero-order release equation,the release profile of the tablets was correlated by least square method,and the correlation coefficient of the equation was used as the index.The single-factor experiment was used to screen the formulation of tri-layer vildagliptin sustained-release tablets.Results The optimized formulation included one drug layer and two outer barrier layers.The barrier layer included HPMC K100M 200 mg,microcrystalline cellulose 198 mg,and magnesium stearate 2 mg.The drug layer consistsed of vildagliptin 100 mg,HPMC K4M 50 mg,microcrystalline cellulose 48 mg,and magnesium stearate 2 mg.The formulation of tri-layer vildagliptin sustained-release tablets met the criteria zero-order release in vitro.Conclusion The tri-layer vildagliptin sustained-release tablets with expected zero-order release are successful developed.