陈颖翀, 周伟成, 雷方方, 黄丽珍, 郑琴, 杨明, 岳鹏飞*. 基于药物晶型结构改善中药活性成分理化特性与功效的研究进展与思考J. 药学学报, 2021,56(8): 2059-2069. doi: 10.16438/j.0513-4870.2021-0813
引用本文: 陈颖翀, 周伟成, 雷方方, 黄丽珍, 郑琴, 杨明, 岳鹏飞*. 基于药物晶型结构改善中药活性成分理化特性与功效的研究进展与思考J. 药学学报, 2021,56(8): 2059-2069. doi: 10.16438/j.0513-4870.2021-0813
CHEN Ying-chong, ZHOU Wei-cheng, LEI fang-fang, HUANG Li-zhen, ZHENG Qin, YANG Ming, YUE Peng-fei*. Research progress and thinking on improving physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine based on crystal structureJ. Acta Pharmaceutica Sinica, 2021,56(8): 2059-2069. doi: 10.16438/j.0513-4870.2021-0813
Citation: CHEN Ying-chong, ZHOU Wei-cheng, LEI fang-fang, HUANG Li-zhen, ZHENG Qin, YANG Ming, YUE Peng-fei*. Research progress and thinking on improving physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine based on crystal structureJ. Acta Pharmaceutica Sinica, 2021,56(8): 2059-2069. doi: 10.16438/j.0513-4870.2021-0813

基于药物晶型结构改善中药活性成分理化特性与功效的研究进展与思考

Research progress and thinking on improving physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine based on crystal structure

  • 摘要: 中药活性成分具有显著的药理活性,在临床疾病治疗中发挥了重大作用。然而,许多中药活性成分存在溶解度低、熔点高和稳定性差等问题,不仅导致其生物利用度低,还限制了其在临床的应用。调控药物晶型结构对改善中药活性成分理化特性或功效具有重要的作用。本文从多晶型、共晶型、无定形/共无定形和纳米晶体等方面总结了几种晶型结构技术在中药活性成分中应用的研究进展,综述了药物晶型结构对中药活性成分理化特性与功效的影响,为中药活性成分创新制剂研究和开发提供依据。

     

    Abstract: The active ingredients in traditional Chinese medicine have been reported to possess significant pharmacological activity and played an important role in clinical treatments. However, lots of the active ingredients in traditional Chinese medicine suffer from disadvantages such as low solubility, high melting point and low stability that results in low bioavailability and limit its clinical application. Crystal structure plays an important role in improving physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine. This review concludes the research advances of several crystal forms used in the active ingredients in traditional Chinese medicine in terms of polymorph, cocrystal, amorphous/coamorphous and nanocrystal. And the effects of crystal forms on the physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine were reviewed. This research may be useful for the formulation preparation and development of the active ingredients in traditional Chinese medicine.

     

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