含聚氧化物、羟丙基甲基纤维素和乙基纤维素的加兰他敏控释片的预处方研究。

IF 5.5 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Andres C Arana-Linares, Paola A Caicedo, María Francisca Villegas-Torres, Andrés F González-Barrios, Natalie Cortes, Edison H Osorio, Constain H Salamanca, Alvaro Barrera-Ocampo
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引用次数: 0

摘要

背景/目的:合理设计缓释基质片需要对颗粒分析、压实行为和药物释放特性有深入的了解。在这项研究中,我们评估了羟丙基甲基纤维素、聚乙烯氧化物和乙基纤维素在加兰他明基质配方中的物理化学、颗粒学和力学性能。方法:光谱(FTIR)和热分析(DSC)证实了药物-聚合物的相容性。我们通过颗粒分析和应用压缩模型(Kawakita, Heckel, Leuenberger)来表征变形机制,评估了流动性、内聚性和通气行为。结果:羟丙基甲基纤维素具有良好的压实性(Tmax = 4.61 MPa)和持续释药(12 h时释药率85.4%,DE% = 62.2%),而聚氧化物具有逐渐侵蚀和一致释药(12 h时释药率88.7%,DE% = 57.5%)。相比之下,乙基纤维素具有较高的黏结性,但基质完整性较差,导致药物提前释放(1 h时为76.6%,DE% = 73.7%)。只有羟丙基甲基纤维素和聚乙烯氧化物配方符合USP标准。结论:这些结果表明,聚合物选择对粉末行为和基质性能有重要影响,强调了在开发稳健的控释系统时需要综合颗粒学和力学评估。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preformulation Study of Controlled-Release Galantamine Matrix Tablets Containing Polyethylene Oxide, Hydroxypropyl Methylcellulose, and Ethylcellulose.

Background/Objectives: 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. Methods: 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. Results: Hydroxypropyl methylcellulose showed superior compactability (Tmax = 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. Conclusions: 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.

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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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