枸橼酸莫沙必利胃内漂浮缓释微丸的制备及体外释放特性考察

Preparation and release characteristics of Mosapride Citrate Intragastric Floating Sustained-release Pellets

目的制备枸橼酸莫沙必利胃内漂浮缓释微丸,并对其体外释药特性进行研究。方法以挤出滚圆法制备枸橼酸莫沙必利胃内漂浮缓释微丸。采用正交设计法,以体外累积释放度和起漂时间为考察指标,优选处方中微晶纤维素、羟丙甲纤维素、乳糖和十八醇的用量。结果制备的胃内漂浮缓释微丸起漂时间短,持续漂浮时间>8 h,且具有显著的缓释性能,体外释药符合Higuchi动力学方程。结论制备的枸橼酸莫沙必利胃内漂浮缓释微丸具有良好的漂浮性能和缓释效果。

Objective To prepare Mosapride Citrate Intragastric Floating Sustained-release Pellets and investigate the drug release mechanism in vitro.Methods Extrusion-spheronization technique was introduced to prepare Mosapride Citrate Intragastric Floating Sustained-release Pellets.The amount of microcrystalline cellulose,hydroxypropyl methylcellulose,lactose and octadecanol were optimized by orthogonal design with accumulative release rate and floating time as the indexes.Results The pellets with short floating time could maintain floating for more than 8 h and had a significant sustained-release profile,the drug in vitro release was in accordance with Higuchi equation.Conclusion The prepared pellets showed a good floating property and sustained-release.