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量身定制的ASD破坏稳定 - - 以基烯基纤维素平衡保质期稳定性和溶解性能
Christian Luebbert1, Edmont Stoyanov2
1amofor GmbH, Otto-Hahn-Str. 15, Dortmund D-44227, Germany.
International journal of pharmaceutics: X
|July 3, 2023
概括
三级无形固体分散 (ASDs) 提高了药物溶解度,但面临一个权衡. 优化聚合物比率的稳定性在含有 fenofibrate 或 simvastatin 的 ASD 中可以降低溶解性能.
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:
- 无形固体分散 (ASDs) 对于水溶性较差的药物至关重要,改善溶解和可溶性.
- 配方开发需要平衡物理稳定性 (防止结晶) 与最佳溶解性能 (高,持续超和).
- 包含两种聚合物的第三级ASD提供了活性药物成分 (API) 的增强稳定和溶解增强的潜力.
研究的目的:
- 为了评估三元性ASD与基烯基纤维素和聚乙烯基合乙烯酸 (PVP VA64) 或基烯基纤维素酸.
- 评估储存期间在这些三元性ASD中无形纤维酸和simvastatin的稳定性.
- 研究聚合物组合对API溶解性能的影响.
主要方法:
- 利用PC-SAFT模型进行热力学预测,以确定最佳的聚合物比率,最大稳定的API负载和聚合物可混合性.
- 进行了三个月的稳定性测试,以验证热力学预测.
- 描述了开发的ASD配方的溶解行为.
主要成果:
- 热力学预测确定了稳定的三元性ASD的最佳聚合物比率和最大API负载.
- 稳定性测试证实了有关ASD稳定性的热力学预测.
- 一个关键的发现是,在热力学上最稳定的ASDs表现出恶化的溶解性能.
- 物理稳定性和溶解性能被发现是研究的聚合物组合中的对立特征.
结论:
- 三级自闭症症具有复杂的配方挑战,最大限度地提高物理稳定性可能会损害溶解性能.
- 选择聚合物组合和比率对于平衡费诺纤维酸和西姆瓦斯塔丁等API的稳定性和溶解至关重要.
- 需要进一步的研究来克服ASD配方中物理稳定性和溶解增强之间的固有权衡.
关键词:
无形固体的分散性固体.结晶化 结晶化 结晶化溶解行为是溶解行为.氧烯基纤维素的含量是多少长期稳定性的长期稳定性混合性 混合性 混合性在PC-SAFT中使用.可溶性 可溶性 溶性超和 超和 超和更多相关视频
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