异质核素在化水晶固体分散的结晶化中的作用
Giovanni López Burgos1, José R Hernández-Espinell2, Tatiana Graciani-Massa2
1Department of Pharmaceutical Sciences, University of Puerto Rico, San Juan, Puerto Rico 00936, United States; Molecular Sciences Research Center, Crystallization Design Institute, University of Puerto Rico, San Juan, Puerto Rico 00926, United States.
聚乙烯二甲 (PET) 涂层的基板加速了乙氨基 (ACM) 在聚乙烯糖醇 (PEG) 中的结晶. 这项研究表明,PET增强了ACM形式II核和在晶体固体分散 (CSD) 中的发生.
科学领域:
- 材料科学 材料科学 材料科学
- 结晶科学 结晶科学
- 制药技术 制药技术 制药技术
背景情况:
- 在化结晶过程中的多态控制,特别是与异质核子,是研究不足的.
- 乙氨基 (ACM) 是一种多态化合物,经常用于制药配方.
- 聚乙烯甘醇 (PEG) 是结晶过程中常见的辅助剂.
研究的目的:
- 为了研究聚乙烯二甲 (PET) 聚合物薄膜对聚乙烯糖醇 (PEG) 中的乙氨基 (ACM) 融化结晶的影响.
- 评估PET涂层基板对ACM核化诱导时间,相位识别和多态形式的影响.
- 探索PET作为异质核剂在晶体固体分散 (CSD) 中控制ACM多态形式的潜力.
主要方法:
- 现场拉曼光谱法用于监测核化诱导时间,并识别ACM-PEG混合物的融化结晶过程中的晶体相.
- 采用X射线衍射 (XRD) 分析PET涂层和未涂层基板上的固化ACM-PEG滴 (囊片) 的首选方向 (PO).
- 在PET涂层基板和未涂层玻璃基板上的结晶之间进行了比较分析.
主要成果:
- 与未涂层基板相比,PET涂层基板在PEG中质量加快了乙氨基II形式 (ACM II) 的核化.
- 当PEG结晶在PET涂层基板上时,PEG中ACM II的发生率平均增加了10%.
- 有证据表明,ACM与PET涂层基板之间可能存在键相互作用,从而促进更快的核形成.
结论:
- 涂PET的基板作为有效的聚合物异质核子,促进选择性结晶的ACM II在PEG.
- 这项研究证明了PET涂层基板的成功实施,通过结晶来加强CSD中ACM的多态控制.
- 这些发现表明,聚合物异质核能剂可以用于基于聚合物的先进配方工艺,以更好地控制药物化合物多态性.
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