药物共晶:一种提高药物理化性质的新兴技术

Diksha Patel, P. Puranik
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引用次数: 6

摘要

新产品开发的主要制约因素是水溶性差、稳定性低、口服生物利用度低、渗透性低。由于世界上销售的大多数药物都是口服给药,并且由于这些生物制药问题,大约40% -50%的新分子实体从未进入市场。因此,与活性药物成分(API)的不良理化性质相关的问题可以使用共结晶方法来解决。结晶技术是提高难溶性药物溶解度的潜在技术,也有助于改善原料药的物理化学性质,同时保留原料药的药理学性质。共晶是由两种或两种以上不同的分子和/或离子化合物组成的晶体单相材料,通常按化学计量比组成,既不是溶剂化物/水合物,也不是简单的盐。它是一个多组件系统,其中一个组件是API,另一个组件称为共流器。共晶体的选择是共晶合成过程中最具挑战性的一步,本文介绍了各种选择共晶体的筛选方法。本文还总结了盐、溶剂化物和水合物共晶的区别,以及共晶的意义和局限性,并简要介绍了不同的共晶形成方法和表征技术。最后,本文重点介绍了85种合成共晶和14种草药共晶及其制备方法和使用的共晶。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pharmaceutical Co-crystal : An Emerging Technique to enhance Physicochemical properties of drugs
Major constraints in development of new product are poor aqueous solubility, stability and low oral bioavailability, low permeability. As majority of drugs marketed worldwide are administered by oral route and about 40% -50% of the new molecular entities were never invade into the market because of such biopharmaceutical issues.So issues related to poor physiochemical property of an active pharmaceutical ingredient (API) can be resolved using co‐ crystallization approach.Crystallization emerge as potential technique for enhancement of solubility of poorly aqueous soluble drugs also helps to improve physicochemical with preserving the pharmacological properties of the API . Cocrystals are solids that are crystalline single-phase materials composed of two or more different molecular and/or ionic compounds generally in a stoichiometric ratio which are neither solvates/hydrates nor simple salts. It is multicomponent system in which one component is API and another is called coformer. Coformer selection is the main challenging step during cocrystal synthesis , so various screening methods for the selection of coformers was explained . This article also summarizes differences between cocrystals with salts, solvates and hydrates along with the implications and limitations of cocrystals .It also provides a brief review on different methods of cocrystal formation and characterization techniuqes of cocrystals. Lastly this article highlights 85 synthetic and 14 herbal cocrystals along with its method of preparation and coformers used.
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