结合实验和计算方法用于三级固体分散,以提高Penfluridol口服生物可用性
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Masoud Mamani1, Gyu Lin Kim1, Su Min Kil1
1College of Pharmacy, Dongguk University, Dongguk-ro-32, Ilsan-Donggu, Goyang 10326, Republic of Korea.
Pharmaceutics
|December 31, 2025
概括
固体分散技术显著改进了penfluridol的使用.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 长期作用的精神分裂症口服抗精神病药物Penfluridol具有较差的水溶性和口服吸收.
- 这些局限性阻碍了它的治疗潜力,尽管它具有有利的剂量计划.
- 固体分散技术为克服这些挑战提供了一个有希望的方法.
研究的目的:
- 为了提高penfluridol的溶解和口服生物可用性.
- 利用固体分散技术改善药物输送.
- 通过机器学习优化penfluridol配方.
主要方法:
- 使用溶剂蒸发制备penfluridol的三元固体分散物.
- 通过随机森林回归建模优化配方成分.
- 在老鼠中评估结构特征,体外药物释放和体内药理动力学.
主要成果:
- 优化的配方 (PF-SD5) 显示,水溶性增加了117倍.
- PF-SD5在1小时内在体外实现了几乎完全的药物释放.
- 在体内研究表明,大鼠的口服生物利用率增加了1.9倍.
- 鉴定证实了载体矩阵内夫的无形状态.
结论:
- 固体分散技术有效地提高了难溶性penfluridol的可溶性和生物利用性.
- 机器学习引导的优化是开发先进药物输送系统的宝贵工具.
- 这一策略有可能提高具有挑战性的药物化合物的治疗疗效.
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