消失和重新出现的多态形态. 本佐卡因:皮克酸系统
J O Henck1, J Bernstein, A Ellern
1Institut für Pharmakognosie der Universität Innsbruck Innrain 52, Josef-Moeller-Haus, 6020 Innsbruck, Austria.
Journal of the American Chemical Society
|July 18, 2001
概括
研究可因 (BC) 和皮克酸 (PA) 系统揭示了结晶难以捉摸的多态形式的方法. 了解热行为是获得转移稳定的晶体结构的关键.
科学领域:
- 晶体学 晶体学是指结晶学.
- 材料科学 材料科学 材料科学
- 化学工程是化学工程的重要组成部分.
背景情况:
- 可因:皮克酸 (BC:PA) 1:1复合物以前表现出一种
- 一个消失的多态形态.
- 一种难以分离的转移稳定的形式.
- 药品共晶体中的多态性对于药物的稳定性和生物可用性至关重要.
研究的目的:
- 为了重新调查本佐卡因:皮克酸 (BC:PA) 系统.
- 为各种BC:PA阶段开发强大的结晶程序.
- 了解结晶转移稳定的多态形式的条件.
主要方法:
- 热显微镜和差分扫描热量计 (DSC) 用于热分析.
- 固态核磁共振 (NMR) 光谱学. 固态核磁共振 (NMR) 光谱学.
- 用于结构确定的X射线晶体学.
- 图集分析用于键的表征.
主要成果:
- 建立了BC:PA系统的相位图.
- 四个不同的晶体相被确定和描述:两个1:1复合物,一个1:1水合物和一个2:1复合物.
- 结构分析揭示了每个阶段的特定结模式.
- 基于热行为开发了结晶转移稳定的形式的策略.
结论:
- 彻底的热分析与热量计方法相结合,使难以获得的转移稳定的多态形态形式的结晶成为可能.
- 了解相位行为对于控制共晶体系统的结晶至关重要.
- 这项研究为访问其他化学系统中的转变稳定多态提供了一个框架.
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