水飞蓟宾缓释胶囊的制备及处方优化

Preparation and Prescription Optimization of Silybin Sustained-release Capsules

目的:制备水飞蓟宾缓释胶囊并优化其处方。方法:减压蒸发法制备水飞蓟宾磷脂复合物(SPC);紫外分光光度法(UV)验证SPC;UV建立水飞蓟宾体外测定方法;单因素法对缓释胶囊内缓释小片骨架材料与填充剂考察;星点设计-效应面法对缓释小片处方优化。结果:成功建立水飞蓟宾的体外测定方法,方法学考察符合要求;SPC最佳药脂比1︰1,复合率78.31%;经验证制出SPC;缓释小片最优处方:水飞蓟宾50%、羟丙甲纤维素K4M(HPMC K4M)33.3%、乙基纤维素(EC)6.7%、微晶纤维素(MCC)10%。结论:制备的缓释胶囊达到设计要求,为制剂进一步开发和临床应用提供参考。

Objective:To prepare silybin sustained-release capsule and optimize its prescription.Methods:Silybin Phospholipid Complex(SPC)was prepared by vacuum evaporation method.SPC was verified by UV.UV method was established for the determination of silybin in vitro.Single factor method was used to study the matrix materials and fillers of sustained-release capsules.The formulation of sustained-release tablets was optimized by the star-point design-effect surface method.Results:The sustained release capsule in vitro determination method were established successfully.The best lipid ratio of SPC was 1︰1,and the compound rate was 78.31%.It verifies to make SPC and it is optimal prescription for sustained-release tablets:silybin 50%,HPMC K4M33.3%,EC 6.7%,MCC 10%.Conclusion:The sustained-release capsules can meet the design requirements and provide reference for the further development of the preparation.