Arana-Linares Andres C, Caicedo Paola A, Villegas-Torres María Francisca, González-Barrios Andrés F, Cortes Natalie, Osorio Edison H, Salamanca Constain H, Barrera-Ocampo Alvaro
Grupo Natura, Departamento de Ciencias Farmacéuticas y Químicas, Facultad Barberi de Ingeniería, Diseño y Ciencias Aplicadas, Universidad Icesi, Calle 18 No. 122-135, Cali 760031, Colombia.
Grupo QBAB, Instituto de Ciencias Aplicadas, Facultad de Ingeniería, Universidad Autónoma de Chile, El Llano Subercaseaux 2801, San Miguel, Santiago 8910060, Chile.
Pharmaceutics. 2025 Aug 30;17(9):1139. doi: 10.3390/pharmaceutics17091139.
: The rational design of modified-release matrix tablets requires a thorough understanding of granulometric analysis, compaction behavior, and drug release profile. In this study, we evaluated the physicochemical, granulometric, and mechanical properties of hydroxypropyl methylcellulose, polyethylene oxide, and ethylcellulose in galantamine matrix formulations. : Spectroscopic (FTIR) and thermal (DSC) analyses demonstrated drug-polymer compatibility. We assessed flowability, cohesion, and aeration behavior through granulometric analysis and applied compressibility models (Kawakita, Heckel, Leuenberger) to characterize deformation mechanisms. : Hydroxypropyl methylcellulose showed superior compactability (T = 4.61 MPa) and sustained drug release (85.4% at 12 h, DE% = 62.2%), while polyethylene oxide enabled gradual erosion and consistent delivery (88.7% at 12 h, DE% = 57.5%). In contrast, ethylcellulose exhibited high cohesiveness but poor matrix integrity, leading to premature drug release (76.6% at 1 h, DE% = 73.7%). Only hydroxypropyl methylcellulose and polyethylene oxide formulations met USP criteria. : These results demonstrate that polymer selection critically influences powder behavior and matrix performance, underscoring the need for integrated granulometric and mechanical evaluation in the development of robust controlled-release systems.
缓释骨架片的合理设计需要全面了解粒度分析、压缩行为和药物释放曲线。在本研究中，我们评估了加兰他敏骨架制剂中羟丙基甲基纤维素、聚环氧乙烷和乙基纤维素的物理化学、粒度和机械性能。：光谱（FTIR）和热分析（DSC）证明了药物与聚合物的相容性。我们通过粒度分析评估了流动性、内聚性和通气行为，并应用压缩性模型（Kawakita、Heckel、Leuenberger）来表征变形机制。：羟丙基甲基纤维素表现出优异的可压缩性（T = 4.61 MPa）和持续药物释放（12小时时为85.4%，DE% = 62.2%），而聚环氧乙烷实现了逐渐侵蚀和持续释放（12小时时为88.7%，DE% = 57.5%）。相比之下，乙基纤维素表现出高内聚性但基质完整性差，导致药物过早释放（1小时时为76.6%，DE% = 73.7%）。只有羟丙基甲基纤维素和聚环氧乙烷制剂符合USP标准。：这些结果表明，聚合物的选择对粉末行为和基质性能有至关重要的影响，强调了在开发稳健的控释系统时进行综合粒度和机械评估的必要性。
