HPMCAS等级对从无形固体分散中释放弱基药物的影响
Pradnya Bapat1, Lynne S Taylor1
1Department of Industrial and Molecular Pharmaceutics, College of Pharmacy, Purdue University, West Lafayette, Indiana 47907, United States.
Molecular pharmaceutics
|December 20, 2024
概括
弱基药物与基甲基纤维素酸盐酸盐 (HPMCAS) 之间的静电相互作用会影响无形固体分散 (ASD) 中的药物释放. 通过增加pH值来降低药物电离,改善了这些ASDs中的药物释放率.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 负电相反的物种可以在水溶液中静电相互作用,从而可能降低溶解度.
- 了解药物聚合物相互作用对于开发稳定的无形固体分散 (ASD) 至关重要.
研究的目的:
- 为了研究脂友弱基药物 (cinnarizine,loratadine) 和基乙酸酸 (HPMCAS) 之间的不溶性复合物形成.
- 了解药物-聚合物静电相互作用如何影响ASDs中的药物和聚合物释放.
- 评估不同HPMCAS等级 (LF,MF,HF) 对释放配置文件的影响.
主要方法:
- 在各种pH条件下进行的表面积规范释放实验.
- 从ASD中测量药物和聚合物释放率.
- 通过量化水相中的聚合物损失来评估复杂化趋势.
主要成果:
- 与HPMCAS-HF的ASD相比,与HPMCAS-LF配制的ASD的释放受到阴离子药物形式的影响较小.
- 增加pH值,减少药物电离,导致药物释放率提高.
- 药物-聚合物静电相互作用显著影响基于HPMCAS的ASD的释放行为.
结论:
- 药物-聚合物静电相互作用在调节基于HPMCAS的ASD药物释放方面发挥着关键作用.
- HPMCAS的等级会影响药物-聚合物复合的程度和随后的释放.
- 进一步的研究应该探索在更复杂的模拟肠液条件下释放.
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