固体药物的多晶型转化和抑制策略

IF 2.6 3区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY CrystEngComm Pub Date : 2024-10-15 DOI:10.1039/D4CE00811A
Yaoguang Feng, Hui Wang, Di Wu, Kui Chen, Na Wang, Ting Wang, Xin Huang, Lina Zhou and Hongxun Hao
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引用次数: 0

摘要

与稳定的结晶形态相比,可迁移形态和无定形形态具有更高的溶解度和溶解速率,因此是低溶解度药物的可行选择。然而,使用易变型和无定形形式可能会导致药物在生产和储存过程中发生多晶型转化,从而降低其生物利用度。首先,讨论了不同的多晶型转化。然后,分析了影响晶体和非晶体稳定性的因素,包括溶剂、温度、湿度和制备工艺。最后,还总结了抑制多晶体转变和非晶体再结晶的策略及其机制,包括合适的储存条件、制备工艺的优化、添加剂的使用、配方的调整以及表面和负载技术。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Polymorph transformation of solid drugs and inhibiting strategies

Metastable forms and amorphous forms exhibit higher solubility and dissolution rates compared to stable crystalline forms, making them viable options for pharmaceuticals with low solubility. However, the use of metastable forms and amorphous forms may result in polymorph transformation in pharmaceutical manufacture and storage, which will reduce their bioavailability. Firstly, different polymorphic transformations were discussed. Then, the factors affecting crystals and amorphous stability, including solvent, temperature, humidity, and preparation processes were analyzed. Finally, strategies and their mechanisms to inhibit polymorphic transformation and amorphous recrystallization were also summarized, including suitable storage conditions, optimization of the preparation processes, use of additives, adjustment of formulation recipes, and surface and loading techniques.

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来源期刊
CrystEngComm
CrystEngComm 化学-化学综合
CiteScore
5.50
自引率
9.70%
发文量
747
审稿时长
1.7 months
期刊介绍: Design and understanding of solid-state and crystalline materials
期刊最新文献
Back cover Back cover Back cover Synthesis of 3D composite materials based on ultrathin LDH nanowalls grown in situ on graphene surface and fast-response NO2 gas sensing performance at room temperature† Variations in crystals of flufenamic acid of its methyl and tert-butyl analogues as impurities as determined by partial dissolutions†
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