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伊特拉科纳无形固体分散物的连续加工策略:聚合物选择和制造技术的影响

Madhuri M Kshirsagar¹, Bandoo C Chatale², Sathish Dyawanapelly¹

¹Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400019, MH, India.

|September 27, 2025

概括

热挤出 (HME) 有效地产生了伊特拉科纳 (ITR) 的无形固体分散 (ASD),显著增强了难以溶解的BCSII类药物的药物释放. 这种连续制造方法为改善口服生物利用性提供了一个可扩展的解决方案.

科学领域:

制药技术制药技术制药技术
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:

像伊特拉可纳 (ITR) 这样的BCSII类药物的水溶性差,限制了口服生物可用性和治疗疗效.
无形固体分散 (ASD) 是一种有前途的策略,可以提高水溶性较差的药物的可溶性和溶解性.
连续制造技术,包括热挤出 (HME) 和喷雾干燥 (SD),为可扩展的ASD生产提供了潜力.

研究的目的:

使用连续制造技术 (HME和SD) 开发和描述伊特拉科纳 (ITR) 的无形固体分散 (ASD).
为了增强ITR的溶解和生物可用性,ITR是一种水溶性较差的BCSII类药物.
评估不同聚合物和制造工艺的适用性,以创建有效的ASD.

主要方法:

基于汉森溶性参数 (HSP) 分析,薄膜造和分子建模的ASD的聚合物选择.
使用HME和SD与Eudragit® EPO,Soluplus®和AQOAT® AS-HG在各种药物与聚合物比率上准备ASD.
使用包括DSC,PXRD,SEM和溶解测试在内的技术对ASD进行全面的表征.

主要成果:

与SD相比,HME表现出卓越的工艺效率,无溶剂操作,以及增强的药物释放.
经过优化,以HME为基础的ASD被制成片剂显示出显著的溶解增强,其中一种配方在2小时内实现了95.88%的ITR释放.
分子建模证实了有利的药物聚合物相互作用,与ASD的稳定性和释放概况的改善相关.

结论:

基于HME的连续制造是一种可扩展和强大的方法,用于生产水溶性较差的药物的ASD.
合理设计ASD配方,整合预测建模和实验选,优化溶解行为.
这种方法有可能改善BCSII类药物的口服治疗结果.

关键词:

无形固体分散的无形固体分散热挤出方式这是伊特拉可纳.可溶性增强提高可溶性喷雾干燥喷雾干燥

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