基于半孔载体的融技术的比较,以改善卡维迪醇溶解
Mila Kovačević1, Amrit Paudel2, Odon Planinšek1
1University of Ljubljana Faculty of Pharmacy, Department of Pharmaceutical Technology, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
概括
高剪切颗粒和热挤出有效地产生了卡维迪洛的无形固体分散 (ASD). HS颗粒体表现出优异的药物释放,证实其适用于增强的卡维迪洛溶解.
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 (ASDs) 增强了难以溶解药物的溶解性和生物可用性.
- 基于化的技术,如热挤出 (HME) 和高剪切 (HS) 颗粒化,对ASD制备有希望.
研究的目的:
- 为了比较使用半孔载体和聚合物矩阵制备卡维迪醇ASD的HS颗粒和HME.
- 评估准备好的ASDs的物理化学特性和溶解性能.
主要方法:
- 使用Syloid® 244FP或Neusilin® US2作为载体和聚乙烯甘醇6000或Soluplus®作为聚合物通过HME和HS化颗粒制备卡维迪醇ASD.
- 使用差分扫描热量计 (DSC),X射线衍射 (XRD),扫描电子显微镜 (SEM) 和溶解测试进行表征.
主要成果:
- 无论是HME和HS粒度都成功地产生了无形的卡维迪醇分散物,DSC和XRD证实了这一点.
- 与HS颗粒相比,HME产生了较大的颗粒,表面更光滑,流动性更好.
- HS颗粒呈现出更粗,更多孔的表面,导致更快的卡维迪醇释放,特别是与Syloid® 244FP.
结论:
- 这两种技术都适合创建无形卡维迪洛尔固体分散.
- 高温溶解颗粒表现出优越的药物释放性能,突出了其开发有效卡维迪醇剂量形式的潜力.
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