使用基于有机酸的固体分散剂来改善溶解的阿尔本达的无形化:一种无溶剂的方法
Nilesh Jambukiya1, Kiran Dudhat2, Sunny Shah1
1B.K. Mody Government Pharmacy College, Polytechnic Campus, Near Ajidam, Rajkot, Gujarat, 360005, India.
AAPS PharmSciTech
|September 11, 2025
概括
这项研究开发了一种无溶剂的方法,使用有机酸来制造阿尔本达 (ABZ) 的固体分散 (SD). 酸显著提高了ABZ的溶解性和溶解性,改善了口服药物递送潜力.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 配方 开发 发展
背景情况:
- 阿尔本达 (ABZ) 具有较差的水溶性和较低的口服生物可用性 (<5%),限制了其治疗功效.
- 增强ABZ溶解对于提高其临床有效性至关重要.
研究的目的:
- 开发一种无溶剂的策略,以使用有机酸的固体分散剂 (SD) 来增强阿尔本达溶解.
- 研究酸 (CA),酸 (TA) 和谷氨酸 (GA) 对ABZ溶解度和固态特性的影响.
主要方法:
- 使用缩酸溶液和干燥来制备ABZ-有机酸固体分散剂.
- 以pH值为依赖的溶解性研究,粉末X射线衍射 (PXRD),FTIR和溶液相1H NMR进行表征.
- 在加速条件下 (40°C/75%RH) 进行阶段溶解研究和稳定性测试.
主要成果:
- 酸 (CA) 增加了188,000倍的ABZ可溶性;在1:1摩尔比率或更高的CA基SD中观察到ABZ的完全无形化.
- 在ABZ和CA之间的键稳定了无形形式和超和.
- 基于CA的SD达到了100%的累积百分比药物溶解 (CPDD) 在0.1N HCl;基于TA的SD达到了80%的CPDD.
结论:
- 使用有机酸 (尤其是CA) 的经济高效,可扩展,无溶剂的方法有效地提高了ABZ的溶解和稳定性.
- 开发的固体分散剂显示了改善阿尔本达等难溶性药物的口服生物可用性的潜力.
- 这种方法为制定其他具有挑战性的疏水性药物提供了有希望的策略.
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