脂在热挤出制备的聚合物固体分散物中药物溶解中的作用
Danilo Monteiro de Carvalho1, Ana Carolina Mendes Lourenço1, Guilherme Gomes Moreira1
1Laboratory of Nanosystems and Drug Delivery Devices (NanoSYS), School of Pharmacy, Universidade Federal de Goiás (UFG), 74605170 Goiânia, GO, Brazil.
ACS omega
|August 4, 2025
概括
豆酸胆 (PPC) 增强固体分散 (SD) 处理和药物溶解,特别是在Soluplus (SLP) 聚合物中. 这种脂质添加改善了像利托纳维尔 (RTV) 这样的溶解不良药物的产量和热处理.
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
背景情况:
- 固体分散 (SDs) 是先进的药物递送系统,聚合物-脂质组合在单一辅助剂使用时得到改善.
- 在SD配方中单独使用时,像copovidone (COP) 和Soluplus (SLP) 这样的水友助剂面临限制.
研究的目的:
- 调查大豆酸丁胆 (PPC) 对药物聚合物SDs溶解性能的影响.
- 评估PPC在含有Ritonavir (RTV) 的SDs的热挤出加工中的作用.
主要方法:
- 固体分散剂 (SDs) 是使用热挤出与利托纳维尔 (RTV) 和copovidone (COP) 或Soluplus (SLP) 制备的.
- 加入了15%和30% (w/w) 度的豆酸胆 (PPC).
- 分析了溶解性能,无形化,工艺产量,形态和颗粒大小.
主要成果:
- 在所有配方中都实现了完整的药物形态化,PPC改善了没有塑化剂的工艺产量.
- 添加PPC影响了水溶中的形态和颗粒大小,表明增强了聚合物-脂质相互作用.
- 基于COP的SD显示RTV溶解的快速增加 (高达7倍);基于SLP的SD显示渐进的增加 (超过5倍).
- PPC 改善了 SLP 基于 SD 的 RTV 溶解,但对 COP 基于 SD 的影响很小.
结论:
- 脂质在SD中的功能取决于药物聚合物相互作用和脂质度.
- 脂的结合促进了SDs的热处理,而不需要额外的辅助剂.
- PPC显示了优化SD配方的潜力,特别是SLP,以改善药物输送.
相关概念视频
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