娑罗子肠溶微丸胶囊的制备及质量评价  

Preparation and Quality Evaluation of Suoluozi Enteric-coated Pellet-based Capsules

作　　者：殷文佳 黄丽华 熊富良 张明 施川 YIN Wenjia;HUANG Lihua;XIONG Fuliang;ZHANG Ming;SHI Chuan(School of Chemistry,Chemical Engineering and Life Sciences,Wuhan University of Technology,Wuhan 430070;Hubei Li Shizhen Pharmaceutical Research Co.,Ltd.,Ezhou 436070;Wuhan Aimin Pharmaceutical Co.,Ltd.,Ezhou 436070)

机构地区：[1]武汉理工大学化学化工与生命科学学院,湖北武汉430070 [2]湖北李时珍药物研究有限公司,湖北鄂州436070 [3]武汉爱民制药股份有限公司,湖北鄂州436070

出　　处：《中国医药工业杂志》2023年第8期1247-1253,共7页Chinese Journal of Pharmaceuticals

基　　金：湖北省科技重大专项项目(2020DEB012);湖北省支持企业技术创新发展项目(2021BAB119)。

摘　　要：采用流化床底喷包衣法,对蔗糖丸芯依次包药物层、隔离层和肠溶衣层,制备娑罗子总皂苷提取物肠溶微丸。以微丸上药率、收率、工艺可行性、七叶总皂苷含量及2 h酸中释放量为评价指标,采用单因素试验结合多指标综合评价法优化肠溶微丸处方。照所得优化处方平行制备3批样品,并测得肠溶微丸的平均粒径为665.26μm,堆密度约为0.92 g/mL,脆碎度低于2.5%,总皂苷含量为(101.30±0.79)%。将所得肠溶微丸装入胶囊后进行体外释放度试验。结果显示,该肠溶微丸胶囊的2 h酸中释放量为(5.26±2.25)%,在磷酸盐缓冲液(pH 6.8)介质中45 min时基本释放完全。The sucrose pill cores were sequentially coated with a drug layer,an isolation layer,and an enteric layer to prepare the enteric-coated pellets loaded with escin from Suoluozi(Semen Aesculi)by bottom spray coating in a fiuidized bed.A single factor test combined with a multi-index comprehensive evaluation method was adopted to optimize the formulation of enteric-coated pellets with the drug loading rate,yield,process feasibility,total escin content,and release amount within 2 h in acidic media as the evaluation indicators.Three batches of Suoluozi enteric-coated pellets were prepared according to the optimal formulation.The average particle size,bulk density,friability and total escin content of the enteric-coated pellets were 665.26μm,0.92 g/mL,below 2.5%,and(101.30±0.79)%,respectively.After filling the obtained enteric-coated pellets into the capsules,an in vitro release test was carried out.The results showed that the release amount of enteric-coated pellet-based capsules within 2 h in acidic media was(5.26±2.25)%,but the drug was basically completely released in phosphate buffer(pH 6.8)in 45 min.

关 键 词：娑罗子(Semen Aesculi) 七叶总皂苷 肠溶微丸 胶囊 底喷包衣 处方优化 质量评价 

分 类 号：R944.5[医药卫生—药剂学]