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非甾体抗炎药物共晶开发中的挑战与进展。

Challenges and Progress in Nonsteroidal Anti-Inflammatory Drugs Co-Crystal Development.

机构信息

Department of Pharmacochemistry, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, Indonesia.

出版信息

Molecules. 2021 Jul 9;26(14):4185. doi: 10.3390/molecules26144185.

Abstract

Co-crystal innovation is an opportunity in drug development for both scientists and industry. In line with the "green pharmacy" concept for obtaining safer methods and advanced pharmaceutical products, co-crystallization is one of the most promising approaches to find novel patent drugs, including non-steroidal anti-inflammatory drugs (NSAID). This kind of multi-component system improves previously poor physicochemical and mechanical properties through non-covalent interactions. Practically, there are many challenges to find commercially viable co-crystal drugs. The difficulty in selecting co-formers becomes the primary problem, followed by unexpected results, such as decreased solubility and dissolution, spring and parachute effect, microenvironment pH effects, changes in instability, and polymorphisms, which can occur during the co-crystal development. However, over time, NSAID co-crystals have been continuously updated regarding co-formers selection and methods development.

摘要

共晶创新为科学家和工业界在药物开发中提供了机会。为了获得更安全的方法和更先进的药物产品,符合“绿色药学”的理念,共晶是寻找新型专利药物的最有前途的方法之一,包括非甾体抗炎药(NSAID)。这种多组分体系通过非共价相互作用改善了先前较差的物理化学和机械性能。实际上,要找到具有商业可行性的共晶药物有很多挑战。共晶形成剂的选择困难成为主要问题,其次是意想不到的结果,例如溶解度和溶解率降低、弹弓效应、微环境 pH 值效应、不稳定性变化和多晶型性,这些在共晶开发过程中都可能发生。然而,随着时间的推移,关于共晶形成剂的选择和方法开发,非甾体抗炎药共晶一直在不断更新。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dcb2/8303568/582516dffe35/molecules-26-04185-g001.jpg

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