固体-液体界面上的共晶体的溶液中介相变:超和生成率和转化途径之间的关系
Runhui Fan1, An Chen1, Yang Yu1
1State Key Laboratory of Natural Medicines, Department of Pharmaceutics, Department of Pharmaceutical Engineering, China Pharmaceutical University, Nanjing 211198, China.
International journal of pharmaceutics
|November 20, 2024
概括
这项研究揭示了在溶解过程中液化基因因 (LQ) 共晶体的新相转换途径. 不同的共晶配方和添加剂,如Eudragit E100影响这些转化,影响药物的溶解性和释放.
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:
- 晶常常面临着溶液介导相变的挑战,这可能会降低它们增强的可溶性.
- 了解这些转变对于优化晶药物递送系统至关重要.
研究的目的:
- 在溶解过程中研究液化基因因 (LQ) 共晶体的新型相位转换途径.
- 根据超和率,探索LQ无水和水合形式的竞争性形成.
- 为了评估添加剂,特别是Eudragit E100对共晶溶解行为的影响.
主要方法:
- 液基因因与尼古丁胺 (LQ-NIC) 和异化物 (LQ-INZ) 的联合结晶.
- 在平面缓冲和含有Eudragit E100的缓冲中进行溶解研究.
- 使用固态特性 (隐含) 分析相变换路径.
主要成果:
- 确定了一个新的场景,其中相变极限扩散到共晶体体中.
- LQ-NIC共晶体表现出多步转化 (共晶 -> 无水化合物LQ -> LQ·H2O),受高超和度的支持.
- 在低超和下,LQ-INZ共晶体表现出一步转化 (共晶 -> LQ·H2O).
- 欧德拉吉特E100通过溶解无水化合物LQ并抑制其转化来改善LQ-NIC溶解,但对LQ-INZ的影响很小.
结论:
- 晶溶解涉及复杂的相变换路径,受到超和生成速率的影响.
- 选择辅助器和添加剂可以调节这些途径,并最终影响药物释放特征.
- 结果为设计稳定和有效的共晶配方提供了关键的见解.
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