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›› 2013, Vol. 13 ›› Issue (5): 862-869.

• 生化工程专栏 • 上一篇    下一篇

快速膜乳化法制备载醋酸曲普瑞林PLGA微球

王宁 王玉霞 秦培勇 韦祎 马光辉   

  1. 北京化工大学生命科学与技术学院 中国科学院过程工程研究所生化工程国家重点实验室 北京化工大学生命科学与技术学院 中国科学院过程工程研究所生化工程国家重点实验室 中国科学院过程工程研究所生化工程国家重点实验室
  • 收稿日期:2013-05-15 修回日期:2013-06-26 出版日期:2013-10-20 发布日期:2013-10-20
  • 通讯作者: 王宁

Preparation of Triptorelin Acetate-loaded PLGA Microspheres by Premix Membrane Emulsification

WANG Ning WANG Yu-xia QIN Pei-yong WEI Yi MA Guang-hui   

  1. College of Life Science and Technology, Beijing University of Chemical Technology State Key Lab of Biochemical Engineering, Institute of Process Engineering, CAS College of Life Science, Beijing University of Chemical Technology State Key Lab of Biochemical Engineering, Institute of Process Engineering, CAS State Key Lab. Biochem. Eng., Inst. Process Eng., Chinese Academy of Sciences
  • Received:2013-05-15 Revised:2013-06-26 Online:2013-10-20 Published:2013-10-20
  • Contact: WANG Ning

摘要: 以生物可降解聚合物聚(乳酸?羟基乙酸)(PLGA)为载体,以160 g/L明胶水溶液为内水相、含500 g/L PLGA的二氯甲烷为油相,采用快速膜乳化和溶剂蒸发法制备了粒径均一的载醋酸曲普瑞林PLGA微球,微球粒径约30 mm,粒径分布系数Span<0.8,醋酸曲普瑞林包埋率达80.12%,药物在磷酸盐缓冲液中释放36 d的释放率为72.60%,体外释放行为良好.

关键词: 醋酸曲普瑞林, 聚(乳酸?羟基乙酸), 微球, 快速膜乳化, 包埋率, 药物释放

Abstract: Triptorelin acetate loaded biodegradable poly(lactic-co-glycolic acid) (PLGA) uniform-sized microspheres were prepared by a method combining premix membrane emulsification and solvent evaporation with high concentration (160 g/L) gelatin as water phase and methylene chloride containing high concentration (500 g/L) PLGA as oil phase. It was possible for the drug completely entrapped by the PLGA microcapsules. The mean diameter of PLGA microspheres was about 30 mm, the encapsulation efficiency of triptorelin acetate 80.12%, and Span (coefficient of size distribution) value less than 0.8. Subsequently, the cumulative release rate of PLGA microspheres loading triptorelin in vitro for 36 d was 72.60%. Furthermore, the release profile of the drug in vitro was well for controlled release.

Key words: triptorelin acetate, poly(lactic-co-glycolic acid), microcapsule, premix membrane emulsification, encapsulation efficienc, drug release

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