Faculty of Engineering and Science, School of Science, University of Greenwich, Chatham Maritime, Chatham, Kent ME4 4TB, UK.
Faculty of Engineering and Science, School of Science, University of Greenwich, Chatham Maritime, Chatham, Kent ME4 4TB, UK.
Adv Drug Deliv Rev. 2017 Aug 1;117:178-195. doi: 10.1016/j.addr.2017.07.008. Epub 2017 Jul 14.
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.
药物共晶是由两个或多个分子组成的多组分体系，通过氢键结合在一起。目前，共晶通过改善活性药物成分 (API) 的物理性质，如可加工性、溶解度、稳定性和生物利用度，为制药行业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新的 API，这对药物开发、监管提交和知识产权保护有重大影响。本文综述了共晶的合成、制造和放大方面的最新趋势和进展。讨论了几种共晶制造技术的操作原理，包括它们在晶体质量、纯度稳定性、产量和大规模生产限制方面的优缺点。
