API佐卡因的相图及其高度持久的,转移稳定的晶体多态
Ivo B Rietveld1,2,3, Hiroshi Akiba1, Osamu Yamamuro1
1Institute for Solid State Physics, University of Tokyo, 5-1-5 Kashiwanoha, Kashiwa 217-8581, Chiba, Japan.
Pharmaceutics
|May 27, 2023
概括
使用热量计和衍射研究了佐卡因多态体. 形式I是最稳定的整体,但形式II仍然是最实用的配方,因为它的室温持久性.
科学领域:
- 固态化学 固态化学
- 材料科学是一种材料科学.
- 晶体学 晶体学是指结晶学.
背景情况:
- 可因表现出三种已知的形式 (I,II和III) 的多态性.
- 形式II和III具有已知的反otropic 阶段关系.
- 形式III在低温和高压下稳定,而形式II在室温下稳定.
研究的目的:
- 研究佐卡因多态 (I,II,III) 的相关系.
- 在不同的条件下确定佐卡因形式的热力学稳定性.
- 将实验数据与in silico晶体结构预测进行比较.
主要方法:
- 阿迪亚巴斯热量测量方法
- 粉末X射线衍射的粉末X射线.
- 高压差分热分析 高压差分热分析
主要成果:
- I型被确定为在室温和高压下最稳定的多态.
- 形式II,虽然不是最稳定的,但在室温下表现出持久性,使其适合配方.
- 形式III在压力-温度相位图中显示单质性,并且缺乏稳定性域.
结论:
- 可因I型是热力学上最稳定的多态.
- 可因形式II是制药配方的首选多态因其在环境条件下的动力稳定性.
- 了解本佐卡因的相位行为对于药物配方和稳定性至关重要.
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