通过开发含有聚合物和表面活性剂的无形固体分散物来增强安福特素B的溶解
Mikayla M Smith-Craven1, Tahnee J Dening1, Anil K Basra1
1Department of Pharmaceutical Chemistry, School of Pharmacy, The University of Kansas, Lawrence, KS 66047, USA.
Journal of pharmaceutical sciences
|May 3, 2024
概括
使用特定表面活性剂开发无形固体分散物 (ASDs) 显著增强口服安福特里辛B (AmB) 溶解. 含有14±2个碳链的硫酸盐表面活性剂的第三级ASD增加了90倍的AmB度.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 氨酸B (AmB) 是一种关键的抗真菌剂,但溶解性差,限制了其临床使用.
- 口服配方是可取的,以改善患者的遵守性和减少副作用.
- 无形固体分散 (ASDs) 是一种有前途的策略,可以提高像AmB.这样的难溶药物的可溶性和生物可用性.
研究的目的:
- 研究表面活性剂对安福特里辛B溶解在无形固体分散物中的影响.
- 为了确定最佳的表面活性物特性 (链长,功能组) 以提高AmB的溶解性.
- 探索辅助剂相互作用在 ASD 三元配方中的作用.
主要方法:
- 使用喷雾干燥开发二元 (AmB:聚合物或AmB:表面活性剂) 和三元 (AmB:聚合物:表面活性剂) ASD.
- 用各种表面活性剂对ASD进行体外溶解测试.
- 使用动态光散射 (DLS) 进行ASD配方的表征.
主要成果:
- 与硫酸盐功能组和碳链长度为14±2个碳的表面活性剂相结合的第三级ASD实现了与晶体AmB相比AmB溶解的90倍增加.
- 具有相同表面活性剂的二进制ASD显示AmB溶解的较低,高达40倍的增加.
- 动态光散射数据表明,三元性ASD中单个,均的粒子大小分布,这表明AmB,聚合物和表面活性剂之间的协同相互作用.
结论:
- 表面活性剂的选择,特别是链条长度和功能组,对于优化ASD中AmB溶解至关重要.
- 三进制ASD配方在二进制系统中表现出优异的性能,这可能是由于协同相互作用阻止AmB自我聚合.
- 这项研究提出了一个可行的策略,用于开发增强的口服安二B配方.
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