聚合物的影响 聚合物对皮拉塞坦聚合物的固态相变的动力学的影响
Fanfan Fan1, Yi Lu1, Shuyuan Xu1
1State Key Laboratory of Natural Medicines, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
聚合物辅料可以通过抑制固态相位过渡来稳定转移稳定的piracetam (PCM) 多态体. 这项研究强调了一种有希望的配方策略,用于提高药物产品的质量和性能.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 物理化学 物理化学
背景情况:
- 活性药物成分 (API) 的元稳定多态提供配方优势,但面临热力学不稳定性.
- 多态不稳定性威胁到药物产品的质量,生物可用性和加工一致性.
- 了解固态相变对于开发稳定的药物配方至关重要.
研究的目的:
- 量化分析piracetam (PCM) 多态固体-固体相变的动力学.
- 为了研究聚合物辅料对PCM多态转化速率的影响.
- 阐明聚合物通过哪些机制影响API中的相变.
主要方法:
- 热阶段显微镜 (HSM) 用于实时观察相变.
- 粉末X射线衍射 (PXRD) 用于定量阶段分析.
- 差分扫描热量计 (DSC) 用于确定聚合物的玻璃过渡温度 (Tg).
主要成果:
- 聚合物显著影响piracetam (PCM) 聚合物的转化速率,特别是在异能转变点 (75°C) 以上.
- 聚烯罗利 (PVP) K30具有最高的玻璃化过渡温度 (Tg),对形式II到形式I过渡表现出最强的抑制作用.
- 聚乙烯甘醇 (PEG),具有最低的Tg,表现出最弱的抑制作用,在低温下,PEG显著降低了形式I到形式II的过渡率.
结论:
- 聚合物辅助剂可以通过抑制固态相位过渡来有效地稳定转移稳定的药物多态体.
- 抑制作用与聚合物细分流动性和结晶界面上的丰富性有关,阻碍了稳定形式的核化和生长.
- 这些发现提供了一个有价值的配方策略,以提高含有转移性多态体的药物产品的稳定性和性能.
更多相关视频
06:55Synthesis of Cyclic Polymers and Characterization of Their Diffusive Motion in the Melt State at the Single Molecule Level
Published on: September 26, 2016
06:26Orientational Transition in a Liquid Crystal Triggered by the Thermodynamic Growth of Interfacial Wetting Sheets
Published on: May 15, 2017
相关概念视频
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Polymer Classification: Crystallinity
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...
Polymer Classification: Stereospecificity
Molecular Weight of Step-Growth Polymers
As the step-growth polymerization involves step-wise condensation of monomers, the molecular weight also builds up eventually. Consequently, high molecular weight polymers are obtained at the late stages of the polymerization, where 99% of monomers have been consumed.
The extent of the...
Polymers
Types of Step-Growth Polymers: Polyesters
Polyesters are commonly prepared from terephthalic acid and ethylene glycol; the crude product is known as poly(ethylene terephthalate) or PET. However, polyesters are synthesized industrially by transesterification of dimethyl terephthalate with ethylene glycol at 150 °C. The two reactants and the...
