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Advanced methodologies for cocrystal synthesis
Advanced Drug Delivery Reviews ( IF 15.2 ) Pub Date : 2017-07-14 , DOI: 10.1016/j.addr.2017.07.008
Dennis Douroumis , Steven A. Ross , Ali Nokhodchi

Pharmaceutical cocrystals are multicomponent systems composed of two or more molecules and held together by H-bonding. Currently, cocrystals provide exciting opportunities in the pharmaceutical industry for the development and manufacturing of new medicines by improving poor physical properties of Active Pharmaceutical Ingredients (APIs) such as processability, solubility, stability and bioavailability. According to the recent reclassification, cocrystals are considered as drug polymorph rather a new API which has a significant impact on drug development, regulatory submissions and intellectual property protection. This review summarizes recent trends and advances in synthesis, manufacturing and scale – up of cocrystals. The operational principles of several cocrystals manufacturing technologies are discussed including their advantages and disadvantages in terms of crystal quality, purity stability, throughput and limitations in large scale production.



中文翻译:

共晶合成的高级方法

药物共晶体是由两个或多个分子组成并通过H键结合在一起的多组分系统。当前,共晶通过改善活性药物成分(API)的不良物理性能,例如可加工性,溶解性,稳定性和生物利用度,在制药工业中为开发和制造新药提供了令人兴奋的机会。根据最近的重新分类,共晶被认为是药物多晶型物,而不是一种新的API,对药物开发,监管文件和知识产权保护具有重大影响。这篇综述总结了共晶的合成,制造和规模化方面的最新趋势和进展。

更新日期:2017-07-14
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