Shi Qin, Moinuddin Sakib M, Cai Ting
State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Acta Pharm Sin B. 2019 Jan;9(1):19-35. doi: 10.1016/j.apsb.2018.08.002. Epub 2018 Aug 16.
In recent years, the coamorphous drug delivery system has been established as a promising formulation approach for delivering poorly water-soluble drugs. The coamorphous solid is a single-phase system containing an active pharmaceutical ingredient (API) and other low molecular weight molecules that might be pharmacologically relevant APIs or excipients. These formulations exhibit considerable advantages over neat crystalline or amorphous material, including improved physical stability, dissolution profiles, and potentially enhanced therapeutic efficacy. This review provides a comprehensive overview of coamorphous drug delivery systems from the perspectives of preparation, physicochemical characteristics, physical stability, and performance. Furthermore, the challenges and strategies in developing robust coamorphous drug products of high quality and performance are briefly discussed.
近年来,共无定形药物递送系统已成为一种用于递送难溶性药物的有前景的制剂方法。共无定形固体是一种单相系统,包含活性药物成分(API)和其他低分子量分子,这些分子可能是具有药理活性的API或辅料。这些制剂相对于纯结晶或无定形材料具有显著优势,包括改善的物理稳定性、溶出曲线以及潜在增强的治疗效果。本文综述从制备、物理化学特性、物理稳定性和性能等方面对共无定形药物递送系统进行了全面概述。此外,还简要讨论了开发高质量和高性能的稳健共无定形药物产品所面临的挑战和策略。