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共晶技术改善非洛地平稳定性及体外溶出度

邹瑶 孟欣 刘梅菊 邢逞 龚宁波 吕扬

医药导报2025,Vol.44Issue(6):867-873,7.
医药导报2025,Vol.44Issue(6):867-873,7.DOI:10.3870/j.issn.1004-0781.2025.06.005

共晶技术改善非洛地平稳定性及体外溶出度

Enhanced Dissolution Behavior and Stability of Felodipine by Cocrystal Technology

邹瑶 1孟欣 1刘梅菊 1邢逞 1龚宁波 1吕扬1

作者信息

  • 1. 北京协和医学院·中国医学科学院药物研究所,晶型药物研究北京市重点实验室,北京 100050
  • 折叠

摘要

Abstract

Objective To develop four novel cocrystals of felodipine aimed at improving its poor solubility.Methods Felodipine-caproamide,felodipine-2,4-dihydroxybenzoic acid,felodipine-2,5-dihydroxybenzoic acid,and felodipine-3,5-dihydroxybenzoic acid cocrystals were prepared using the slurry method.The cocrystals were characterized by powder X-ray diffraction(PXRD),differential scanning calorimetry(DSC),thermogravimetric analysis(TGA),and Fourier-transform infrared spectroscopy(FT-IR).Stability tests and in vitro dissolution studies were conducted to assess their pharmaceutical properties.Results All four cocrystals demonstrated improved solubility and dissolution rates compared to pure felodipine.Notably,the felodipine-3,5-dihydroxybenzoic acid cocrystal showed superior stability and a marked increase in solubility.Conclusion Cocrystallization technology significantly enhanced the stability and dissolution profile of felodipine,underscoring its potential for pharmaceutical formulation development.

关键词

非洛地平/共晶/晶体工程/溶出度/溶出速率

Key words

Felodipine/Cocrystal/Crystal engineering/Dissolution degree/Dissolution rate

分类

药学

引用本文复制引用

邹瑶,孟欣,刘梅菊,邢逞,龚宁波,吕扬..共晶技术改善非洛地平稳定性及体外溶出度[J].医药导报,2025,44(6):867-873,7.

基金项目

北京市自然科学基金资助项目(7222261) (7222261)

中国医学科学院医学与健康科技创新工程资助项目(2022-I2M-01-015). (2022-I2M-01-015)

医药导报

OA北大核心

1004-0781

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