The Effects of Polymorphism on Physicochemical Properties and Pharmacodynamics of Solid Drugs.
The Effects of Polymorphism on Physicochemical Properties and Pharmacodynamics of Solid Drugs.
复制标题
多晶型对固体药物理化性质和药效学的影响。
DOI：
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发表时间：
2018
影响因子：
3.1
通讯作者：
Xin Huang
中科院分区：
文献类型：
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作者：
Yanan Zhou;Jingkang Wang;Yan Xiao;Ting Wang;Xin Huang
背景
目前，固体材料的多晶性在医药、食品、精细化工等领域发挥着重要的作用。由于晶体结构的不同，不同晶型的固体药物表现出不同的物理化学性质，这可能导致药物的生物利用度和半衰期不同。固体药物的晶型研究已成为药物剂型设计、审批、生产和质量控制中不可缺少的重要组成部分。
方法
为了揭示多态之间的差异，本文概述和讨论了多态的分类方法和每一类的特点。详细讨论了多态对固体药物的粉末性质、熔点、熔化热、溶出行为和稳定性等物理化学特性的影响。此外，还总结和讨论了药物生物利用度和多晶型疗效的各种差异。
结果
由于内部晶体结构的不同，同一固体药物的不同晶型通常表现出不同的物理化学性质，包括粉末性质、熔点、熔化热、溶出行为和稳定性。此外，不同晶型的固体药物往往发挥不同的疗效。
结论
作为影响固体药物质量和疗效的重要因素之一，药物物质的多态现象在药学领域的研究已有50多年的历史。大量研究表明，对多晶性的全面了解对固体药物的开发、剂型设计、批准、生产、质量控制和疗效具有重要意义。
BACKGROUND
Nowadays, the polymorphism of solid materials plays important roles in pharmaceutical field, food industry, fine chemicals and so on. Due to the differences in crystal structure, different polymorphs of a given solid drug show different physicochemical characteristics, which may lead to different drug bioavailability and half-life of the drug. Studies about polymorphism of solid drugs have become an indispensable important component in dosage form design, approval, production and quality control of drugs.
METHODS
In order to reveal the dissimilarity between polymorphs, the classification approach of polymorphism and the features of each category are outlined and discussed in this paper. The influence of polymorphism on physicochemical characteristics of solid drugs such as powder property, melting point, enthalpy of fusion, dissolution behavior and stability are discussed in detail. Furthermore, a variety of differences in drug bioavailability and curative effect of polymorphs are also summarized and discussed.
RESULTS
Due to the differences in internal crystalline structure, different polymorphs of the same solid drugs generally show different physicochemical properties, including powder property, melting point, enthalpy of fusion, dissolution behavior and stability. Furthermore, different polymorphs of solid drugs often exert a diverse curative effect.
CONCLUSION
As one of the significant factors to affect the quality and curative effect of solid drugs, polymorphism of drug substances has been investigated in the pharmaceutical field for over 50 years. Considerable studies indicate that comprehensive understanding of polymorphism is important for development, dosage form design, approval, production, quality control and curative effect of solid drugs.