Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, 576 104, India.
AAPS PharmSciTech. 2020 Nov 8;21(8):309. doi: 10.1208/s12249-020-01849-z.
Solid dispersion is the preferred technology to prepare efficacious forms of BCS class-II/IV APIs. To prepare solid dispersions, there exist a wide variety of polymeric carriers with interesting physicochemical and thermochemical characteristics available at the disposal of a formulation scientist. Since the advent of the solid dispersion technology in the early 1960s, there have been more than 5000 scientific papers published in the subject area. This review discusses the polymeric carrier properties of most extensively used polymers PVP, Copovidone, PEG, HPMC, HPMCAS, and Soluplus® in the solid dispersion technology. The literature trends about preparation techniques, dissolution, and stability improvement are analyzed from the Scopus® database to enable a formulator to make an informed choice of polymeric carrier. The stability and extent of dissolution improvement are largely dependent upon the type of polymeric carrier employed to formulate solid dispersions. With the increasing acceptance of transfer dissolution setup in the research community, it is required to evaluate the crystallization/precipitation inhibition potential of polymers under dynamic pH shift conditions. Further, there is a need to develop a regulatory framework which provides definition and complete classification along with necessarily recommended studies to characterize and evaluate solid dispersions.
固体分散体是制备 BCS 类 II/IV API 有效形式的首选技术。为了制备固体分散体,有各种各样的具有有趣物理化学和热化学特性的聚合物载体可供制剂科学家使用。自 20 世纪 60 年代初固体分散体技术问世以来,该领域已经发表了 5000 多篇科学论文。本综述讨论了固体分散体技术中最广泛使用的聚合物 PVP、共聚维酮、PEG、HPMC、HPMCAS 和 Soluplus®的聚合物载体特性。从 Scopus®数据库中分析了关于制备技术、溶解和稳定性改进的文献趋势,以使制剂师能够明智地选择聚合物载体。稳定性和溶解程度的提高在很大程度上取决于用于制备固体分散体的聚合物类型。随着转移溶解装置在研究界越来越被接受,需要评估聚合物在动态 pH 变化条件下对结晶/沉淀的抑制潜力。此外,需要制定一个监管框架,为固体分散体提供定义和完整的分类以及必要的推荐研究,以进行表征和评估。