Garg Utsav, Azim Yasser
Department of Applied Chemistry, Zakir Husain College of Engineering & Technology, Faculty of Engineering & Technology, Aligarh Muslim University Aligarh 202002 Uttar Pradesh India
RSC Med Chem. 2021 Feb 9;12(5):705-721. doi: 10.1039/d0md00400f. eCollection 2021 May 26.
The focus of the review is to discuss the relevant and essential aspects of pharmaceutical cocrystals in both academia and industry with an emphasis on non-steroidal anti-inflammatory drugs (NSAIDs). Although cocrystals have been prepared for a plethora of drugs, NSAID cocrystals are focused due to their humongous application in different fields of medication such as antipyretic, anti-inflammatory, analgesic, antiplatelet, antitumor, and anti-carcinogenic drugs. The highlights of the review are (a) background of cocrystals and other solid forms of an active pharmaceutical ingredient (API) based on the principles of crystal engineering, (b) why cocrystals are an excellent opportunity in the pharma industry, (c) common methods of preparation of cocrystals from the lab scale to bulk quantity, (d) some latest case studies of NSAIDs which have shown better physicochemical properties for example; mechanical properties (tabletability), hydration, solubility, bioavailability, and permeability, and (e) latest guidelines of the US FDA and EMA opening new opportunities and challenges.
本综述的重点是讨论药物共晶体在学术界和工业界的相关重要方面,重点是非甾体抗炎药(NSAIDs)。尽管已经为大量药物制备了共晶体,但NSAID共晶体受到关注是因为它们在不同药物领域有大量应用,如退烧药、抗炎药、镇痛药、抗血小板药、抗肿瘤药和抗癌药。本综述的要点包括:(a)基于晶体工程原理的共晶体及活性药物成分(API)其他固体形式的背景;(b)为什么共晶体是制药行业的一个绝佳机遇;(c)从实验室规模到批量制备共晶体的常用方法;(d)一些NSAIDs的最新案例研究,这些研究显示出更好的物理化学性质,例如机械性能(可压性)、水合作用、溶解度、生物利用度和渗透性;以及(e)美国食品药品监督管理局(FDA)和欧洲药品管理局(EMA)的最新指南带来的新机遇和挑战。