多晶型、共晶、溶剂化物和盐等多种形式是药物的固体存在形式,多晶型的存在直接导致外观、熔点、溶解度等多种理化性质差异化。药物共晶能够在不改变药物结构的情况下调整药物包括吸湿性,溶出速率、稳定性、生物利用度,以及依从性等,达到改善治疗的最终目标。香兰素作为一种天然辅助香料,具有辅助抑菌、稳定剂、共晶形成物等作用,因其与API具有较强的氢键倾向,是共晶制备的常用共晶形成体,被广泛用于药物共晶。基于近年来对香兰素多晶型及共晶的研究进展,分别阐述了香兰素单晶多晶型、制备方法、共晶机理及药物共晶,及其应用。还强调了香兰素作为药物共晶形成物的一些实例,以说明共晶结构对活性药物成分的理化性质、机械性能、生物利用度等各个方面的影响。本文旨在归纳总结香兰素多晶型及共晶的最新研究进展,为其进一步发展提供参考。
Polymorphism, cocrystals, solvates and salt are the solid forms of drugs. The existence of polymorphism directly leads to the differentiation of physical and chemical properties such as appearance, melting point and solubility. Pharmaceutical cocrystals can adjust hygroscopicity, dissolution rate, stability, bioavailability, and compliance without changing drug structure to achieve the ultimate goal of improving treatment. Vanillin, as a natural auxiliary flavor, has the functions of auxiliary bacteriostasis, stabilizer and eutectic formation. Due to its stronger hydrogen bond tendency with API, vanillin is a common eutectic formation in eutectic preparation and is widely used in drug eutectic. Based on the research progress of vanillin polycrystalline and eutectic in recent years, the single crystal vanillin polycrystalline, preparation method, eutectic mechanism and drug eutectic application are described, and some new techniques for crystallization are introduced. Some examples of vanillin as drug eutectic were also highlighted to illustrate the influence of eutectic structure on physicochemical properties, mechanical properties and bioavailability of active drug ingredients. This paper aims to summarize the latest research progress of vanillin polycrystalline and eutectic and provide reference for its further development.
Polymorphism, cocrystals, solvates and salt are the solid forms of drugs. The existence of polymorphism directly leads to the differentiation of physical and chemical properties such as appearance, melting point and solubility. Pharmaceutical cocrystals can adjust hygroscopicity, dissolution rate, stability, bioavailability, and compliance without changing drug structure to achieve the ultimate goal of improving treatment. Vanillin, as a natural auxiliary flavor, has the functions of auxiliary bacteriostasis, stabilizer and eutectic formation. Due to its stronger hydrogen bond tendency with API, vanillin is a common eutectic formation in eutectic preparation and is widely used in drug eutectic. Based on the research progress of vanillin polycrystalline and eutectic in recent years, the single crystal vanillin polycrystalline, preparation method, eutectic mechanism and drug eutectic application are described, and some new techniques for crystallization are introduced. Some examples of vanillin as drug eutectic were also highlighted to illustrate the influence of eutectic structure on physicochemical properties, mechanical properties and bioavailability of active drug ingredients. This paper aims to summarize the latest research progress of vanillin polycrystalline and eutectic and provide reference for its further development.
唐 宏,王 杨,黄小容,陈虹洁,黄承洪. 香兰素多晶型及共晶研究进展Polymorphism and Cocrystal Research Progress of Vanillin[J]. 材料科学, 2022, 12(02): 112-122. https://doi.org/10.12677/MS.2022.122012
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