无形固体分散:API和助剂的制备方法和物理化学性质的影响
Varun Kushwah1, Cecilia Succhielli1, Isha Saraf1
1Research Center Pharmaceutical Engineering GmbH, 8010 Graz, Austria.
Pharmaceutics
|August 29, 2024
概括
这项研究表明,Soluplus® (SOL) 聚合物和高玻璃过渡温度 (Tg) 活性药物成分 (API) 增强无形固体分散稳定性. 热挤出 (HME) 略高于喷雾干燥 (SD),但加工是关键.
科学领域:
- 制药科学 制药科学
- 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 (ASDs) 对于提高难溶性药物的可溶性和生物利用性至关重要.
- 热挤出 (HME) 和喷雾干燥 (SD) 等制造方法显著影响ASD特性.
- 了解聚合物-药物相互作用和加工效应对于稳定的ASD配方至关重要.
研究的目的:
- 研究不同聚合物和制造方法 (HME和SD) 对ASD固态特性,稳定性和制药性能的影响.
- 评估药物负载 (20%和30%) 对自闭症特征的影响.
- 评估加速稳定条件对ASD物理化学性质的影响.
主要方法:
- 用HME和SD编制二进制ASD,使用不同的药物负载.
- 使用X射线散射 (WAXS) 和调制差分扫描热量计 (mDSC) 进行固态性质的表征.
- 通过红外 (IR) 和拉曼光谱来研究分子相互作用;评估体外药物释放和加速稳定性.
主要成果:
- 基于Soluplus® (SOL) 的ASD表现出比基于基甲基纤维素 (HPMC) 的ASD更高的稳定性.
- 具有高玻璃过渡温度 (Tg) 的ASD和显示强烈聚合物相互作用的API显示出增强的稳定性.
- 融挤出ASD比喷雾干燥 (SD) ASD稍微稳定,尽管下处理影响了API结晶.
结论:
- 聚合物选择 (SOL与HPMC) 和API特性 (高Tg,强相互作用) 对ASD稳定性至关重要.
- 制造方法 (HME与SD) 对稳定性有适度的影响,加工诱导的结晶是关键考虑因素.
- 颗粒物特性显著影响无形固体分散的整体性能和稳定性.
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