溶剂电螺旋无形固体分散剂含有高伊特拉科纳,赛莱科克西布,梅本达和费诺纤维酸盐的药物加载和释放潜力
Jana Becelaere1, Olmo Frateur1, Ella Schoolaert1
1Ghent University, Department of Materials, Textiles and Chemical Engineering, Faculty of Engineering and Architecture, Technologiepark 70A, B-9052 Ghent, Belgium.
概括
这项研究表明,使用电旋转用于溶解不良药物的超高药物载荷无形固体分散 (ASD) 方法. 该技术增强了药物的溶解性和稳定性,显示了生物制药分类系统II类药物的广泛适用性.
科学领域:
- 材料科学 材料科学 材料科学
- 制药技术 制药技术 制药技术
- 药物运输 药物运输 药物运输
背景情况:
- 溶性较差的药物往往具有较低的口服生物可用性.
- 无形固体分散 (ASDs) 是提高溶解性的有希望的策略.
- 发展具有高药物负载的自闭症仍然具有挑战性.
研究的目的:
- 为了证明使用溶剂电旋转的超高药载ASD的可行性.
- 调查药物聚合物相互作用在实现高药物负载中的作用.
- 评估ASDs的溶解增强和物理稳定性.
主要方法:
- 难以溶解的药物 (伊特拉科纳,梅本达,切莱科西布,纤维酸盐) 的溶剂电与聚合物 (聚-2-乙基-2-佐林,聚烯皮罗利).
- 不同的聚合物度低于可旋转的极限,以达到高药含量.
- 使用调制差分扫描热度计 (mDSC) 和X射线衍射 (XRD) 进行表征.
- 非沉没溶解测试以评估可溶性增强.
主要成果:
- 在多种难溶药物中,达到多达80%的药物含量的ASD.
- 证明了范德瓦尔斯相互作用,除了键,有助于高药物负载.
- 实验混合性预测与弗洛里-哈金斯理论一致.
- 与结晶形式相比,可溶性增加了多达50倍.
- 聚二乙烯二氧化) 有效抑制了药物沉,增强了稳定性.
结论:
- 电是一种多功能技术,用于生产具有超高药物负载的物理稳定的ASD.
- 开发的ASD显著提高了生物制药分类系统II类药物的可溶性和溶解率.
- 这种方法提供了一种可行的策略,用于提高难以溶解的化合物的生物利用性.
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