制剂开发和优化艺术 - - 卢姆法林自纳米乳化药物输送系统的配方开发和优化
T R Mudyahoto1, O A Omoteso1, S M Khamanga1
1Division of Pharmaceutics, Faculty of Pharmacy, Rhodes University, Makhanda 6139, South Africa.
Die Pharmazie
|August 15, 2025
概括
开发新的自我纳米乳化药物递送系统 (SNEDDS) 显著提高了阿尔特梅瑟 (ART) 和卢梅林 (LMF) 的可溶性和口服生物可用性. 这些优化的配方表现出快速释放药物和高负载能力.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术 纳米技术
背景情况:
- 较差的水溶性限制了利波菲尔药物的口服吸收和生物可用性,例如甲醇 (ART) 和粉素 (LMF).
- 自行纳米乳化药物输送系统 (SNEDDS) 为克服溶解性挑战提供了一个有希望的方法.
研究的目的:
- 为ART和LMF制定和优化油入水 (o/w) SNEDDS.
- 为了提高这些脂性药物的可溶性,溶解率和口服生物可用性.
主要方法:
- 使用平衡溶解性研究和伪三次相图来选择最佳的辅助剂.
- 实验设计指导了SNEDDS的制造和优化.
- 描述包括滴滴大小分析,负载能力和体外药物释放研究.
主要成果:
- 油酸 (OA) 显示了对ART和LMF的高溶解能力.
- 克雷莫福® EL (CEL) 和Transcutol® HP (THP) 被确定为有效的表面活性剂和辅助表面活性剂.
- 优化的SNEDDS表现出纳米尺寸的液滴,两种药物的负载能力>99%,在15分钟内释放药物的>95%.
结论:
- 开发的O/W SNEDDS显著改善了ART和LMF的溶解率和程度.
- 这种配方策略有可能提高难溶性药物的口服生物可用性.
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