对联合喷雾干燥的梅洛西卡姆与奇托桑和溶解剂的溶解增强的机制性见解
Tereza Vařilová1, Petra Svačinová2, Karl G Wagner3
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Charles University, Akademika Heyrovského 1203/8, Hradec Králové, 500 05, Czech Republic.
Scientific reports
|December 14, 2025
概括
与酸盐 (CHIT) 和酸 (SLS) 联合喷雾干燥梅洛西卡姆 (MX) 显著提高了溶解率. 这种可扩展的配方方法提高了难溶性药物的生物制药性能.
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:
- 溶解不良的药物在实现充分的生物可用性方面存在重大挑战.
- 梅洛西卡姆 (MX) 是一种非类固醇抗炎药物,具有较低的水溶性,限制了其治疗疗效.
- 提高药物溶解对于改善这种化合物的体内性能至关重要.
研究的目的:
- 开发和评估一种联合喷雾干燥技术,以提高梅洛西卡姆 (MX) 的溶解率.
- 调查酸盐 (CHIT) 和酸硫酸盐 (SLS) 作为三元配方中的功能辅助剂的作用.
- 评估开发的联合喷雾干燥方法的可扩展性和工业适用性.
主要方法:
- 使用小型和中型喷雾干燥机准备了MX,CHIT和SLS的三级配方.
- 同喷雾干燥产品与物理混合物和原始MX进行了比较.
- 进行了体外溶解测试,以评估药物释放概况.
- 固态特征使用了X射线粉末衍射 (XRPD),里埃变换红外光谱 (FTIR) 和共聚焦拉曼显微镜.
主要成果:
- 同喷雾干燥显著增加了MX的溶解率,在5分钟内达到80%的释放率.
- 固态分析表明MX结晶性和药物辅助剂相互作用的微妙变化.
- 确定的关键机制包括减少MX聚合,通过SLS提高产品的可湿性,增加矩阵的水友性.
结论:
- 与CHIT和SLS一起喷雾干燥是一种有效和可扩展的策略,用于增强MX等难溶药物的溶解.
- 该方法提供了一种强大的方法来提高药物的生物制药性能.
- 配方过程通过与药物溶液一起喷CHIT分散来简化,避免需要溶解.
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