College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, No. 1200, Cai Lun Road, Pudong District, Shanghai 201203, PR China.
Engineering Research Center of Modern Preparation Technology of Traditional Chinese Medicine of Ministry of Education, Shanghai University of Traditional Chinese Medicine, No. 1200, Cai Lun Road, Pudong District, Shanghai 201203, PR China.
Carbohydr Polym. 2023 Jul 1;311:120731. doi: 10.1016/j.carbpol.2023.120731. Epub 2023 Feb 27.
Hydroxypropyl methylcellulose (HPMC) is an important polymeric excipient. Its versatility in terms of molecular weights and viscosity grades is the basis for its wide and successful application in the pharmaceutical industry. Low viscosity grades of HPMC (like E3 and E5) have been used as physical modifiers for pharmaceutical powders in recent years due to their unique physicochemical and biological properties (e.g., low surface tension, high T, strong hydrogen bonding ability, etc.). Such modification is the co-processing of HPMC with a drug/excipient to create composite particles (CPs) for the purpose of providing synergistic effects of functional improvement as well as of masking undesirable properties of the powder (e.g., flowability, compressibility, compactibility, solubility, stability, etc.). Therefore, given its irreplaceability and tremendous opportunities for future developments, this review summarized and updated studies on improving the functional properties of drugs and/or excipients by forming CPs with low-viscosity HPMC, analyzed and exploited the improvement mechanisms (e.g., improved surface properties, increased polarity, hydrogen bonding, etc.) for the further development of novel co-processed pharmaceutical powders containing HPMC. It also provides an outlook on the future applications of HPMC, aiming to provide a reference on the crucial role of HPMC in various areas for interested readers.
羟丙基甲基纤维素(HPMC)是一种重要的聚合物赋形剂。其分子量和黏度级别的多样性是其在制药工业中广泛成功应用的基础。近年来,由于具有独特的物理化学和生物学特性(例如低表面张力、高 Tg、强氢键结合能力等),低黏度级别的 HPMC(如 E3 和 E5)已被用作药物粉末的物理改性剂。这种改性是将 HPMC 与药物/赋形剂共加工,以形成复合颗粒(CPs),目的是提供功能改善的协同效应以及掩盖粉末的不良性质(例如流动性、可压缩性、可压缩性、溶解度、稳定性等)。因此,鉴于其不可替代性和巨大的发展潜力,本综述总结并更新了通过与低黏度 HPMC 形成 CPs 来改善药物和/或赋形剂功能特性的研究,分析和利用了改善机制(例如,改善表面性质、增加极性、氢键等),以进一步开发含有 HPMC 的新型共加工药物粉末。它还展望了 HPMC 的未来应用,旨在为感兴趣的读者提供有关 HPMC 在各个领域的关键作用的参考。