通过薄膜造对口服里托纳维尔无形固体分散物的聚合物的选
Ayse Nur Oktay1,2, James E Polli2
1Department of Pharmaceutical Technology, Gulhane Faculty of Pharmacy, University of Health Sciences, Ankara 06018, Türkiye.
Pharmaceutics
|November 27, 2024
概括
这项研究选了聚合物以检测里托纳维尔的无形固体分散 (ASD),确定HPMCAS-L和PVP-VA作为有希望的候选物. 这些聚合物增强了药物溶解和生物可用性,为ASD发展提供了资源高效的方法.
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:
- 无形固体分散 (ASD) 增强了难溶性药物的口服生物可用性.
- 药物聚合物相互作用和可混合性对于ASD的形成和表现至关重要.
研究的目的:
- 使用计算和实验方法,选聚合物以检测利托纳维尔潜在的ASD.
- 通过ASD配方识别合适的聚合物,以改善口服里托纳维尔的生物可用性.
主要方法:
- 使用汉森溶解度参数,弗洛里-哈金斯参数和玻璃过渡温度进行计算选.
- 实验性表征包括药物溶解性,沉抑制,显微镜,DSC,溶解能力和溶解研究.
- 通过薄膜造为七种聚合物制备ASD:EudragitS100,HPMCAS-L,HPMCAS-H,HPMCAS L:H,PEG-6000,PVP-VA和Soluplus.
主要成果:
- 鉴定出HPMCAS-L,HPMCAS L:H,Soluplus和PVP-VA是里托纳维尔抗ASD的潜在聚合物.
- 在不同的药物负载中,HPMCAS-L和PVP-VA表现出一致的可行性 (20%和40%).
- 与单独的无形药物相比,所有识别的聚合物都改善了里托纳维尔的溶解;计算方法预测了PEG-6000和EudragitS100的不利结果.
结论:
- HPMCAS-L和PVP-VA是利托纳维尔发展ASD的首选聚合物.
- 这项研究支持在ASD发展过程中采用节约资源的聚合物选择方法.
- 有效的聚合物查对于优化药物输送和生物可用性至关重要.
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