通过KinetiSol将聚合物混合物预处理成聚合物合金,可以增加Ivacaftor无形固体分散药物加载和溶解
Stephen A Thompson1, Daniel A Davis2, Dave A Miller2
1Molecular Pharmaceutics and Drug Delivery Division, College of Pharmacy, The University of Texas at Austin, 2409 W. University Ave, PHR 4.214, Austin, TX 78712, USA.
Biomedicines
|May 27, 2023
概括
在无形固体分散 (ASD) 配方之前创建聚合物合金可以增强药物加载和溶解. 与传统混合物相比,将聚合物预加工成单相合金提高了 ivacaftor ASD 的性能.
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:
- 无形固体分散 (ASDs) 对于改善难溶性药物的生物可用性至关重要.
- 传统的ASD配方通常在药物负载和物理稳定性方面面临限制.
- 将聚合物预加工成合金提供了一种新的方法来克服这些局限性.
研究的目的:
- 研究形成单相聚合物合金对无形固体分散特性的影响.
- 为了比较用聚合物合金制成的ASD与聚合物混合物的性能.
- 为了评估药物负载,溶解,稳定性和分子相互作用.
主要方法:
- 使用KinetiSol化合物,制造出高烯酸乙酸糖和povidone聚合物合金.
- 使用聚合物合金,未经加工的聚合物混合物和单个聚合物制备Ivacaftor ASD.
- 描述包括无形性,溶解测试,里埃变换红外光谱学和固态核磁共振.
主要成果:
- 用聚合物合金ASD实现了50% (w/w) ivacaftor的更高药物负载,而其他组合则达到40%.
- 聚合物合金ASD在模拟肠液中6小时后显示出33%的更高溶解度.
- 合金中的povidone和ivacaftor之间的改变键解释了增强的溶解.
结论:
- 形成单相聚合物合金是一种可行的策略,可以增强ASD特性.
- 聚合物合金的预处理允许量身定制的材料特性,改善药物加载,溶解和稳定性.
- 这种技术为开发先进的无形固体分散提供了一个有前途的途径.
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