药物-聚合物相互作用的相互作用和释放性能对于基于HPMCAS的无形固体分散的相互作用
Pradnya Bapat1, Shubhajit Paul2, Yin-Chao Tseng2
1Department of Industrial and Molecular Pharmaceutics, College of Pharmacy, Purdue University, West Lafayette, Indiana 47907, United States.
Molecular pharmaceutics
|February 12, 2024
概括
药物化学显著影响无形固体分散 (ASD) 的药物释放. 阴离子药物与HPMCAS等聚合物形成不溶性复合物,阻碍自闭症药物释放.
科学领域:
- 制药科学 制药科学
- 聚合物化学 聚合物化学
- 药物运输 药物运输 药物运输
背景情况:
- 无形固体分散 (ASD) 对于提高药物的溶解性和生物可用性至关重要.
- 在ASD中药物分子和聚合物之间的相互作用是复杂的,并影响药物释放动力学.
- 了解这些药物聚合物相互作用对于设计有效的药物输送系统至关重要.
研究的目的:
- 调查药物化学对基甲基纤维素酸糖酸盐 (HPMCAS) 基ASDs药物释放的影响.
- 探索静电相互作用和复杂化在调节药物释放中的作用.
- 建立药物聚合物复合体形成和释放性能之间的关系.
主要方法:
- 使用表面积正常化溶解以评估药物释放率.
- 采用共同沉实验来量化药物形成与HPMCAS不溶性复合物的倾向.
- 研究了pH值和药物电离对复合物的形成和释放的影响.
主要成果:
- 从基于HPMCAS的ASD中释放的药物根据不溶性复合物形成的程度进行了分类.
- 中性或阳离子药物在pH值6.8时显示出足够的释放,即使在更高度.
- 阴离子药物与HPMCAS形成不溶性复合物,导致自闭症药物释放不良.
- 一种弱基本药物在ASD中的电离状态下表现出减少释放,与其作为整洁无形药物的行为相反.
结论:
- 在HPMCAS和脂友性阴阳性药物之间的静电相互作用促进不溶性复合体的形成.
- 这种复杂性显著损害了含有这种药物的ASD的释放性能.
- 定制药物聚合物相互作用对于优化ASD药物释放至关重要.
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