沙库巴曲缬沙坦钠缓释片的制备与释药机制研究  

Preparation and release mechanism of sacubitril/valsartan sustained-release tablets

作　　者：程曼曼 施沁青 王菁华 尹莉芳 秦超 韩晓鹏 CHENG Man-man;SHI Qin-qing;WANG Jing-hua;YIN Li-fang;QIN Chao;HAN Xiao-peng(Department of Pharmaceutics,School of Pharmacy,China Pharmaceutical University,Nanjing 210009)

机构地区：[1]中国药科大学药学院药剂系,南京210009

出　　处：《中南药学》2021年第5期801-807,共7页Central South Pharmacy

基　　金：国家自然科学基金资助项目(No.81871477)。

摘　　要：目的制备沙库巴曲缬沙坦钠缓释片,并研究其体外释药机制。方法以HPMC K100LV和HPMC K4M为骨架材料,以2、6、8 h累积释放度为考察指标,在单因素考察的基础上运用中心复合设计-效应面法优化处方,并对最优处方进行释药机制研究。结果最优处方组成为沙库巴曲/缬沙坦400 mg,HPMC K100LV 18%,HPMC K4M 7%,无水乳糖 25%,硬脂酸镁 1.5%,微粉硅胶 1.5%。缓释片体外释药符合一级动力学特征,药物以扩散和骨架溶蚀相结合的双重机制进行释放。结论本研究制备的缓释片制备工艺简单,具有良好的体外缓释特征。Objective To prepare sacubitril/valsartan sustained-release tablets and determine their in vitro drug release mechanism.Methods Sacubitril/valsartan sustained-release tablets were prepared by HPMC K100LV and HPMC K4M as the matrix materials.Cumulative release degree at 2,6,and 8 h was used as the dependent variables.The optimal formulation of the sustained-release tablets was predicted via central composite experimental design.The in vitro drug release mechanism of sacubitril/valsartan sustained-release tablets was studied.Results The optimal formulation included sacubitril/valsartan(400 mg),HPMC K100LV(18%),HPMC K4M(7%),lactose(25%),magnesium stearate(1.5%)and microsilica gel(1.5%).The in vitro dissolution of the sustained-release tablets followed the first order release model,with the dual mechanism of diffusion and matrix erosion.Conclusion The sustained-release tablets prepared show good sustained drug release effect and the preparation process is simple.

关 键 词：沙库巴曲缬沙坦钠 缓释片 中心复合设计-效应面法 释药机制 

分 类 号：R944.9[医药卫生—药剂学]