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共结晶方法的进展综述及其筛选、制剂和表征简述。

A review on advancement of cocrystallization approach and a brief on screening, formulation and characterization of the same.

作者信息

Sakhiya Dhruv C, Borkhataria Chetan H

机构信息

Gujarat Technological University (GTU) Nr.Vishwakarma Government Engineering College Nr.Visat Three Roads, Visat - Gandhinagar Highway Chandkheda, Ahmedabad, 382424, Gujarat, India.

Department of Pharmaceutics, B. K. Mody Government Pharmacy College, Rajkot, India.

出版信息

Heliyon. 2024 Apr 1;10(7):e29057. doi: 10.1016/j.heliyon.2024.e29057. eCollection 2024 Apr 15.

Abstract

The objective of this review is, to discuss recent advancements in screening methods for co-formers, evaluation cum confirmation methods and co-crystallization with examples. Co-crystals are considered as a new form of an old drug entity. Co-crystals improve the stability, hygroscopicity, solubility, dissolution, and physicochemical properties of pure drugs without altering chemical and pharmacological properties. Advancement in co-crystal formulation methods like electrospray and laser-irradiation methods are showing potential for solvent-free co-crystallization and tends to give better yield and lesser loss of materials. Screening methods are also transformed from trial and error to in-silico methods, which facilitate the selection process by reducing the time of screening and increasing the number of co-formers to be screened. Advanced evaluation methods like Raman and solid-state NMR spectroscopy provide a better understanding of crystal lattice by pinpointing the interaction between drug/co-former molecules. The same evaluation methods can also differentiate between the formation of salt and co-crystals. Co-crystals are helping open a new door in pharmaceutical industries in the field of formulation for the improvement of physicochemical properties in existing old molecules and several new molecules. With a motto of "making a good drug better", co-crystals show scope for vast research and give researchers an ocean of opportunities to make the impossible, possible.

摘要

本综述的目的是通过实例讨论共形成物筛选方法、评估及确证方法以及共结晶方面的最新进展。共晶体被视为旧药物实体的一种新形式。共晶体可改善纯药物的稳定性、吸湿性、溶解度、溶出度及理化性质,而不改变其化学和药理性质。诸如电喷雾和激光辐照法等共晶体制备方法的进展显示出无溶剂共结晶的潜力,且往往能提高产率并减少物料损失。筛选方法也从试错法转变为计算机辅助方法,这通过减少筛选时间和增加待筛选共形成物的数量促进了选择过程。诸如拉曼光谱和固态核磁共振光谱等先进的评估方法通过确定药物/共形成物分子之间的相互作用,能更好地理解晶格结构。同样的评估方法还能区分盐和共晶体的形成。共晶体正助力在制药行业为改善现有旧分子及多种新分子的理化性质的制剂领域打开一扇新的大门。秉持“让好药更好”的宗旨,共晶体展现出广阔的研究空间,并为研究人员提供了大量机会,使不可能变为可能。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/21d2/11004889/4c3190f66f22/gr1.jpg

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