通过热挤出和喷雾干燥制备的无形固体分散物的稳定性和再结晶
Dominik Martynek1, Luděk Ridvan2, Mia Sivén3
1Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 5, 166 28 Prague 6, Dejvice, Czech Republic; Zentiva, k.s., Ukabelovny 130, 10237 Prague 10, Czech Republic.
International journal of pharmaceutics
|February 11, 2025
概括
喷雾干燥和热挤出产生无形固体分散 (ASD). 热挤出提供了更好的稳定性,而喷雾干燥提高了溶解率,PVP K30的性能优于HPMC E5.5.
科学领域:
- 制药技术 制药技术 制药技术
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 无形固体分散 (ASD) 对于提高难溶性药物的可溶性和生物利用性至关重要.
- 喷雾干燥 (SD) 和热挤出 (HME) 是ASD的主要制造技术.
- 了解SD和HME的比较性能对于优化药物产品开发至关重要.
研究的目的:
- 为了比较评估通过喷雾干燥和热挤出制备的基于印莫他辛的ASD的稳定性和溶解性能.
- 评估聚合物类型 (PVP K30与HPMC E5) 对ASD特征的影响.
- 研究ASD在加速储存条件下 (温度和湿度升高) 的行为.
主要方法:
- 使用PVP K30和HPMC E5.5的喷雾干燥和热挤出来制备印莫他辛ASD.
- 包括物理状态分析和固态特性在内的综合分析性表征.
- 内在溶解率 (IDR) 的测量.
- 在压力条件下的再结晶稳定性研究.
主要成果:
- 与喷雾干燥的对应物相比,热挤出的ASD显示出对再结晶的优越物理稳定性.
- 喷雾干燥的ASD表现出明显更高的内在溶解率.
- PVP K30在增强印美他素ASD的溶解速率和物理稳定性方面比HPMC E5更有效.
结论:
- 在喷雾干燥和热挤出之间做出选择会影响ASD稳定性和溶解性能之间的平衡.
- PVP K30 是一种首选的聚合物辅助剂,用于开发稳定有效的印梅他辛无形固体分散剂.
- 这些发现为优化ASD制造过程提供了有价值的见解,以优化难溶药物的制造过程.
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