Guo Minshan, Sun Xiaojie, Chen Jiahui, Cai Ting
State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Acta Pharm Sin B. 2021 Aug;11(8):2537-2564. doi: 10.1016/j.apsb.2021.03.030. Epub 2021 Mar 23.
Pharmaceutical cocrystals are multicomponent systems in which at least one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients. Cocrystallization of a drug substance with a coformer is a promising and emerging approach to improve the performance of pharmaceuticals, such as solubility, dissolution profile, pharmacokinetics and stability. This review article presents a comprehensive overview of pharmaceutical cocrystals, including preparation methods, physicochemical properties, and applications. Furthermore, some examples of drug cocrystals are highlighted to illustrate the effect of crystal structures on the various aspects of active pharmaceutical ingredients, such as physical stability, chemical stability, mechanical properties, optical properties, bioavailability, sustained release and therapeutic effect. This review will provide guidance for more efficient design and manufacture of pharmaceutical cocrystals with desired physicochemical properties and applications.
药物共晶体是多组分体系,其中至少有一种组分是活性药物成分,其他组分是药学上可接受的成分。药物与共形成剂的共结晶是一种有前景的新兴方法,可用于改善药物的性能,如溶解度、溶出曲线、药代动力学和稳定性。本文综述全面概述了药物共晶体,包括制备方法、物理化学性质及应用。此外,还重点介绍了一些药物共晶体的实例,以说明晶体结构对活性药物成分各个方面的影响,如物理稳定性、化学稳定性、机械性能、光学性能、生物利用度、缓释和治疗效果。本综述将为更高效地设计和制造具有所需物理化学性质及应用的药物共晶体提供指导。