通过循环德克斯特林复合增强里瓦洛克萨班的药物释放和物理化学性质:全面的分析方法
Cristina Solomon1, Valentina Anuța2, Iulian Sarbu3
1Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 6 Traian Vuia St., 020956 Bucharest, Romania.
Pharmaceuticals (Basel, Switzerland)
|June 27, 2025
概括
这项研究使用环氧德克斯纳入复合物和冷化增强了里瓦罗克萨班的溶解性. 由此产生的配方表现出更好的稳定性和溶解性,与商用Xarelto相美.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 物理化学 物理化学
背景情况:
- 里瓦罗克萨班具有较差的水溶性,限制了其生物利用率和治疗效率.
- 口服抗凝剂需要改进的配方策略,以增强药物输送.
- 环极素被广泛用于提高难溶性药物的可溶性.
研究的目的:
- 为了增强里瓦洛克萨班的溶解性和溶解特性.
- 通过使用循环德克斯特林衍生物来制备稳定的里瓦罗克萨班纳入复合物.
- 为了研究循环德克斯含和冷化的协同效应.
主要方法:
- 使用β-cyclodextrin (β-CD),methyl-β-cyclodextrin (Me-β-CD) 和hydroxypropyl-β-cyclodextrin (HP-β-CD) 形成包含复合物.
- 热化技术用于复杂的制备和稳定.
- 使用FTIR,SEM,XRD和TGA进行物理化学表征.
主要成果:
- FTIR证实了里瓦洛克萨班在环极素中的非共价相互作用和封装.
- SEM和XRD显示了转变为一个有孔的,无形的矩阵,药物的晶度降低.
- TGA表明,包含复合物的热稳定性得到了改善.
- 药理技术评估表明,它具有适合直接压缩的特性.
结论:
- 循环德克斯的纳入复合物和冷化协同增强了里瓦罗克萨班的溶解性和溶解性.
- 开发的配方与纯利瓦洛克萨班相比,具有更好的特性.
- 这些策略为开发有效的里瓦洛克萨班固体剂型提供了潜力.
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