无水 quercetin 和聚合物物理混合物的可溶性优于无形固体分散物的可溶性
Xu Ma1,2, Hong Su2, Yongming Liu3
1College of Chemistry and Materials Science, Fujian Normal University Fuzhou 350117 Fujian China.
RSC advances
|March 28, 2025
概括
素 (QUE) 和聚合物的物理混合物显示出比无形固体分散 (ASD) 更好的溶解性. 这是因为ASD中的凝状相隔阻碍了QUE的释放,这是物理混合物中避免的问题.
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:
- 奎尔 (QUE) 是一种具有水溶性差的黄类化合物,限制了其生物利用性.
- 无形固体分散 (ASD) 是提高溶解度的一种策略,但对 QUE 的研究是有限的.
- 在ASD溶解期间的凝状相分离可以阻碍药物释放.
研究的目的:
- 在物理混合物和ASD与聚合物的溶解性和溶解行为调查quercetin.
- 了解凝状相分离对ASDs中的奎尔素释放的影响.
- 确定改善水溶性较差的化合物的可溶性策略,如Que.
主要方法:
- 无水 QUE 与聚烯 (PVP) 和 Soluplus 的物理混合物和 ASD 的制备.
- 不同配方中的Que的可溶性研究.
- 溶解测试用于评估QUE释放配置文件.
- 在溶解过程中对凝状相分离的分析.
主要成果:
- 与PVP或Soluplus混合的QUE的物理混合物比相应的ASD具有更高的溶解度.
- 在 QUE ASD 溶解过程中观察到显著的凝状相分离,特别是在 Soluplus 中,减少了 QUE 的释放.
- QUE与聚合物的物理混合物没有表现出这种类似凝的相位分离.
- 将一个转移稳定的多态与一个聚合物的组合可能是面临ASD相关阶段分离问题的溶解不良药物的可行方法.
结论:
- 物理混合物优于ASDs,可以改善氨酸溶解度,当凝状相分离是一个问题时.
- 在ASD溶解期间的凝状相分离显著阻碍了水溶性较差的药物的释放.
- 在这种情况下,利用与聚合物结合的转变稳定多态体提供了一个有希望的策略,以克服可溶性挑战.
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