表面成分和湿度对高药载荷无形分散配方的溶解性能的重要性
Tze Ning Hiew1, Marina A Solomos2, Prapti Kafle2
1Department of Industrial and Molecular Pharmaceutics, College of Pharmacy, Purdue University, West Lafayette, Indiana 47907, United States.
Journal of pharmaceutical sciences
|September 30, 2024
概括
改进无形固体分散 (ASD) 配方涉及克服低药物负载的挑战. 这项研究表明,通过表面修饰来增强颗粒可湿性是提高高药载荷ASD药物释放性能的关键.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 化学工程是化学工程的重要组成部分.
背景情况:
- 无形固体分散 (ASD) 受到低药物负载的限制,特别是对于需要显著的聚合物稳定性的疏水性药物.
- 疏水性药物表现出不良的湿透性,阻碍药物释放,并需要先进的配方策略.
- 研究了一种层次粒子方法,以提高高药负载自闭症患者的表现.
研究的目的:
- 调查粒子表面组成,可湿性和ASD中药物释放之间的关系.
- 评估一个层次化的粒子方法,以提高药物加载和溶解性能.
- 确定ASD配方中疏水性药物的最佳表面修饰策略.
主要方法:
- 采用了格拉索普雷维尔 (药物) 和高乙酸 (聚合物) 作为模型系统.
- 通过溶剂蒸发和共沉产生高药载荷的ASD,然后通过二次辅助剂进行表面修饰.
- 使用两阶段溶解,接触角测量,SEM和XPS来评估释放,可湿性,形态和表面组成的粒子的特征.
主要成果:
- 用水友性聚合物进行表面修饰并不能始终保证药物释放的改善.
- 接触角测量显示,次要辅助剂对颗粒可湿性的显著影响.
- 具有增强的可湿性颗粒显示出与可湿性较差的颗粒相比,药物释放率更高的颗粒,无论药物负载如何.
结论:
- 颗粒的可湿性是影响无形固体分散配方性能的一个关键因素.
- 层次粒子方法为开发具有增强溶解特性的高药载荷自闭症症提供了一个有希望的策略.
- 对于表面修饰的二次助剂的战略选择对于优化ASDs的可湿性和药物释放至关重要.
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