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将高通量ASD查与rDCS结合起来,以简化难溶药物的开发

Malte Bøgh Senniksen¹, Nicole Wyttenbach², Susanne Page³

¹Fraunhofer Institute for Translational Medicine and Pharmacology, Theodor-Stern-Kai 7, 60596 Frankfurt am Main, Germany; Pharmaceutical R&D, F. Hoffmann-La Roche Ltd., Grenzacherstrasse 124, 4070 Basel, Switzerland.

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

|May 18, 2025

概括

这项研究引入了一种新方法,将高通量无形固体分散 (ASD) 查与精细的可开发性分类系统 (rDCS) 结合起来,以改善口服药物配方. 这种方法有效地提高了难溶性活性药物成分 (API) 的生物可用性.

科学领域:

制药科学制药科学
药物运输药物运输药物运输
制定发展制定发展

背景情况:

活性药物成分 (API) 的水溶性和溶解率差,限制了口服生物可用性.
无形固体分散 (ASD) 是一种关键的配方策略,可以增强药物吸收.
系统性评估将体外ASD查与体内生物可用性联系起来是具有挑战性的.

研究的目的:

为了证明一种简化方法来制定作为ASDs的不溶性API.
将高通量ASD查与改进的可开发性分类系统 (rDCS) 整合起来.
评估聚合物载体对API溶解和生物可用性潜力的影响.

主要方法:

采用聚合物选用于无形药物稳定 (SPADS) 方法来快速准备ASD电影.
研究了三种API (贝菲图皮坦,塞莱科西布,伊特拉科纳) 与八种聚合物载体的溶解性能.
利用完善的可开发性分类系统 (rDCS) 来分类API及其ASD配方.

主要成果:

溶解的API度受到聚合物载体和药物负载的选择的显著影响.
尤德拉吉特E,HPMC 100LV和Soluplus对所研究的API产生了有利的载体效应.
ASD配方在rDCS分类中表现出有利的转变 (例如,从IIb到I类),表明吸收潜力有所改善.

结论:

结合SPADS和rDCS的方法有效地简化了不易溶解的API在ASD中的配方.
这种新的方法促进了直接比较和明智选择,使得配方策略成为可能.
综合系统为预测和改善药物的生物可用性提供了一个强大的工具.

关键词:

无形固体的分散.解散解散解散解散高通量选的高通量选口服吸收口服吸收精制的可开发性分类系统 (rDCS)超和超和超和

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