在口服配方中预测目标药物颗粒大小,使用精制的可开发性分类系统 (rDCS)
Kristian Beran1,2, Eline Hermans2, René Holm3
1Fraunhofer Institute of Translational Medicine and Pharmacology, 60596 Frankfurt am Main, Germany.
Pharmaceutics
|July 29, 2023
概括
新的方程有助于确定可溶性较差的药物的最佳颗粒大小减小,以改善口服吸收. 这解决了溶解的局限性,确保药物有效地透肠壁.
科学领域:
- 制药科学 制药科学
- 药物输送和配方 药物输送和配方
背景情况:
- 溶解限制可能会阻碍口服药物吸收,特别是溶解性较差的化合物,如果溶解时间超过肠道运输或肠壁透率.
- 减少药物颗粒大小是克服这些溶解挑战的常见策略.
研究的目的:
- 开发和验证一套新的方程,用于计算必要的颗粒大小减小,以克服溶解限制的口服吸收.
- 基于完善的可开发性分类系统 (rDCS) 框架.
主要方法:
- 基于完善的可开发性分类系统 (rDCS) 开发新的方程.
- 应用这些方程来计算特定药物物质的目标粒子半径 (rtarget).
- 使用三个案例验证:沃里康纳,莱博雷克桑和伊斯特拉德菲林.
主要成果:
- 方程允许根据可用的数据计算适当的颗粒大小减小.
- 对于lemorexant (rDCS Class I),预计半径≤20μm可以增强吸收.
- 对于伊斯特拉迪菲林 (rDCS IIb类),计算了大约12微米的目标半径.
结论:
- 开发的方程提供了一种定量方法,以确定改善口服吸收所需的颗粒大小减小.
- 结果与现有文献一致,表明方程适用于不同类型的rDCS中的不同药物物质.
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