根据热挤出热模的热调节,在共晶和同形形式之间切换
Peiya Shen1, Chunfeng Zhang2, Enshi Hu1
1School of Pharmacy, China Pharmaceutical University, Nanjing 211198, P. R. China.
Molecular pharmaceutics
|May 30, 2023
概括
热挤出选择性地通过调整桶温度来产生印美甲 - 尼古丁胺胺共晶 (CC) 或共形 (CM) 配方. 这些配方提高药物的溶解性和稳定性,与单独的印米他辛相比.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 绿色化学 绿色化学
背景情况:
- 晶 (CC) 和共形 (CM) 技术是提高药物的溶解性和生物可用性的绿色方法.
- 热挤出 (HME) 是一种无溶剂,可扩展的制造技术,适用于CC和CM生产.
研究的目的:
- 使用HME选择性地制备印美他辛-尼古丁胺胺 (IMC-NIC) CC和CM配方.
- 研究IMC-NIC CC和CM的形成机制.
- 评估已制备的配方的溶解和稳定性.
主要方法:
- 热挤出 (HME) 在不同的桶温度 (105-150°C).
- 固态核磁共振 (SS NMR) 光谱学. 固态核磁共振.
- 辐射分布函数 (RDF) 和结合能量 (Ebind) 的计算.
主要成果:
- 通过调节HME桶温度来实现IMC-NIC CC (105-120 °C) 和CM (125-150 °C) 的选择性制备.
- 通过SS NMR,RDF和Ebind的计算,在较低温度下通过强异构相互作用和有序结构阐明了CC的形成,在较高温度下通过较弱相互作用和无序结构阐明了CM的形成.
- 与晶体或无形IMC相比,IMC-NIC CC和CM都显示出更好的溶解和稳定性.
结论:
- HME提供了一种简单,环保的方法,用于调节CC和CM配方的制备.
- 桶温度是控制IMC-NIC配方分子排列和性能的关键参数.
- 开发的战略提供了一种灵活的方法来提高药物的溶解性和稳定性.
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