天然产物研究与开发 ›› 2019, Vol. 31 ›› Issue (7): 1271-1277.doi: 10.16333/j.1001-6880.2019.7.022

• 开发研究 • 上一篇    下一篇

柚皮素自微乳不对称膜渗透泵胶囊的制备及体外评价

王章姐*,刘自平,许燕,尹伟   

  1. 安徽新华学院药学院,合肥 230088
  • 出版日期:2019-07-29 发布日期:2019-07-29
  • 基金资助:

    安徽高校自然科学研究项目(KJ2016A312)

Preparation and in vitro evaluation of naringenin self-microemulsifying osmotic pump capsule

WANG Zhang-jie*,LIU Zi-ping,XU Yan,YIN Wei   

  1. School of Pharmaceutical Sciences of Anhui Xinhua College,Hefei 230088,China
  • Online:2019-07-29 Published:2019-07-29

摘要: 制备柚皮素自微乳不对称膜渗透泵胶囊并考察其体外释药行为。实验利用球晶技术进行自微乳的固化研究,以醋酸纤维素浓度、栓模浸入聚合物溶液中时间、栓模浸入淬火液中时间为自变量,采用星点设计-效应面优化法,以囊壳厚度和24 h药物累积释放度为因变量,确定不对称膜渗透泵胶囊壳的最佳制备工艺。其最佳制备工艺为:醋酸纤维素浓度9.44%,栓模浸入聚合物溶液中时间3.77 min,栓模浸入淬火液中时间15.86 min,按最佳工艺得到的药物累积释放度为96.27%,囊壳厚度为0.275 mm。体外释药行为符合零级释药方程(R=0.999 7)。柚皮素自微乳不对称膜渗透泵胶囊可有效控制药物缓慢释放,解决难溶性药物制成渗透泵制剂释药不完全的问题。

关键词: 柚皮素, 自微乳, 不对称膜, 渗透泵胶囊, 星点设计

Abstract: To prepare naringenin self-microemulsion asymmetric membrane osmotic pump capsule and investigate its drug release behavior in vitro.The solidification of self-microemulsion was studied by using spherical crystallization technique.Cellulose acetate concentration,time for immersed in polymer solution and quenching liquid of the mold were selected as independent variables.The optimal preparation process of the asymmetric membrane osmotic pump capsule shell was determined by using the star design-effect-surface optimization method,taking the envelope thickness and 24h drug cumulative release as the dependent variables.The optimal preparation technologies of asymmetric membrane osmotic pump capsule shell were determined as follows:The cellulose acetate concentration was 9.44%.The time of the mold in the polymer solution and the quenching liquid was 3.77 and 15.86 min respectively.The cumulative drug release was 96.27%,and capsule shell thickness was 0.275 mm in the optimal preparation technology of asymmetric membrane osmotic pump capsule shell.The drug delivery behavior in vitro conforms to the zero-order drug delivery equation (R=0.999 7).Naringenin self-microemulsion asymmetric membrane osmotic pump capsule can slow down the release of drugs and solve the incomplete release of osmotic pump preparations made from insoluble drugs.

Key words: naringenin, self-microemulsifying, asymmetric membrane, osmotic pump capsule, central composite design

中图分类号: 

R944.9