School of Pharmacy, Jiangsu Vocational College of Medicine, Yancheng 224005, China; Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
School of Pharmacy, Jiangsu Vocational College of Medicine, Yancheng 224005, China.
Int J Pharm. 2020 Nov 30;590:119925. doi: 10.1016/j.ijpharm.2020.119925. Epub 2020 Oct 2.
Compared to their crystalline forms, amorphous pharmaceutical solids present marvelous potential and advantages for effectively improving the oral bioavailability of poorly water-soluble drugs. A central issue in developing amorphous pharmaceutical solids is the stability against crystallization, which is particularly important for maintaining their advantages in solubility and dissolution rate. This review provides a comprehensive overview of recent studies focusing on the physical stability of amorphous pharmaceutical solids affected by nucleation, crystal growth, phase separation and the addition of polymers. Moreover, we highlight the novel technologies and theories in the field of amorphous pharmaceutical solids. Meanwhile, the challenges and strategies in maintaining the physical stability of amorphous pharmaceutical solids are also discussed. With a better understanding of physical stability, the more robust amorphous pharmaceutical formulations with desired pharmaceutical performance would be easier to achieve.
与结晶形式相比，无定形药物固体具有显著的潜力和优势，可有效提高水溶性差的药物的口服生物利用度。开发无定形药物固体的一个核心问题是对结晶的稳定性，这对于保持其在溶解度和溶解速率方面的优势尤为重要。本综述全面概述了最近的研究，重点关注受成核、晶体生长、相分离和聚合物添加影响的无定形药物固体的物理稳定性。此外，我们还强调了无定形药物固体领域的新技术和理论。同时，还讨论了保持无定形药物固体物理稳定性的挑战和策略。通过更好地了解物理稳定性，可以更容易地实现具有所需药物性能的更稳健的无定形药物制剂。
