在半孔中药物负载对无形稳定性和性能的影响
Christoffer G Bavnhøj1, Matthias M Knopp2, Korbinian Löbmann3
1Pharmaceutical Development, H. Lundbeck A/S, DK-2500 Copenhagen, Denmark.
Pharmaceutics
|February 24, 2024
概括
在干燥的条件下,半孔有效地稳定无形赛莱科西布在孔隙填充能力 (PFC) 下18个月. 在PFC上加载导致再结晶,影响溶解配置和超和.
科学领域:
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
背景情况:
- 半孔二氧化 (MS) 在药物封装方面进行研究.
- 在多发性硬化中,药物负荷较高可能导致无形药物形式的身体不稳定.
研究的目的:
- 评估MS中药物负载水平对无形赛莱可西布稳定性和溶解的影响.
- 调查在毛孔填充容量 (PFC) 下面,在毛孔填充容量 (PFC) 下面和在毛孔填充容量 (PFC) 上方的药物负载.
主要方法:
- 在MS ParteckSLC500.上确定单分子负载能力 (MLC) 和PFC的赛莱科西布.
- 在准备和18个月的加快储存 (40°C,干燥/潮湿) 后分析了含药的MS配方.
- 评估无形形态的稳定性和溶解概况.
主要成果:
- 当负载低于PFC (<48.4%重量%) 并且存储干燥时,MS保存了无形赛莱科克西布18个月.
- 在PFC中加载导致即使在干燥条件下也能进行再结晶.
- 所有样品在潮湿条件下重新结晶.
- 新鲜制备的配方显示超和;低于PFC的负载实现了比PFC (DS ~ 6) 更高的超和 (DS ~ 15).
- 存储后保持稳定的无形配方表现出不变的释放配置文件.
结论:
- 在干燥条件下,半孔可以在PFC以下保持无形赛莱科西布的稳定性.
- 在PFC的湿度和负载会损害无形药物稳定性.
- 药物加载会影响超和和溶解,而较低的负载可以提高性能.
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