聚合物物理化学特征对酸在固体分散中的无形化和结晶化的影响
Seda Arioglu-Tuncil1,2, Lisa J Mauer2
1Department of Nutrition and Dietetics, Necmettin Erbakan University, Meram, Konya 42090, Türkiye.
Polymers
|February 13, 2025
概括
这项研究调查了聚合物如何在无形固体分散中防止酸结晶. 碳甲基纤维素和pectin是最有效的,聚合物相互作用和特性影响稳定性.
科学领域:
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
- 物理化学 物理化学
背景情况:
- 无形固体分散对于提高难溶性药物的可溶性和生物利用性至关重要.
- 酸是一种常见的辅助剂,可以结晶,影响配方的稳定性.
- 了解聚合物辅助剂相互作用是开发稳定的无形配方的关键.
研究的目的:
- 研究酸在各种聚合物的固体分散中的形态化和结晶.
- 确定聚合物物理化学性质对无形酸稳定性的影响.
- 建立一个聚合物排名,以抑制酸结晶.
主要方法:
- 酸-聚合物混合物的冷化.
- 在受控的温度和湿度下储存分散物.
- 使用粉末X射线衍射,差分扫描热度计和里埃变换红外光谱学进行分析.
- 确定水分吸附异热量和含量的方法.
主要成果:
- 在特定的聚合物度下,用CMC-Na,PEC,GG,GEL,HPMC和KG成功形成了无形酸分散.
- 酸结晶在所有分散在54%的RH,和KG分散在32%的RH.
- 聚合物在抑制结晶的有效性按照以下顺序进行:CMC-Na > PEC ≥ GEL > HPMC > GG > KG.
结论:
- 聚合物的特性,如分子间相互作用,碳基,玻璃过渡温度 (Tg) 和高度,显著影响无形酸的稳定性.
- CMC-Na和PEC在维持无形酸方面非常有效.
- 最佳的聚合物选择对于创建稳定的无形固体分散非常重要.
相关概念视频
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
279
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
279
Polymer Classification: Crystallinity
2.8K
Unlike ionic or small covalent molecules, polymers do not form crystalline solids due to the diffusion limitations of their long-chain structures. However, polymers contain microscopic crystalline domains separated by amorphous domains.
Crystalline domains are the regions where polymer chains are aligned in an orderly manner and held together in proximity by intermolecular forces. For example, chains in the crystalline domains of polyethylene and nylon are bound together by van der Waals...
Crystalline domains are the regions where polymer chains are aligned in an orderly manner and held together in proximity by intermolecular forces. For example, chains in the crystalline domains of polyethylene and nylon are bound together by van der Waals...
2.8K
Factors Influencing Drug Absorption: Pharmaceutical Parameters
113
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
113
Factors Influencing Drug Absorption: Physicochemical Parameters
208
The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
208
Factors Affecting Dissolution: Particle Size and Effective Surface Area
681
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
681
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
171
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
171


