通过优化基于分子相互作用机制的聚合物和表面活性剂来增强里瓦罗克萨班载荷微球的口服生物利用性
Min-Jong Choi1, Mi Ran Woo2, Kyungho Baek1
1Department of Pharmaceutical Engineering, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan 31116, South Korea.
Molecular pharmaceutics
|July 11, 2023
概括
用聚乙烯 (PVP) 和酸 (SLS) 配制的微球显著提高了里瓦洛克萨班 (RXB) 的溶解性,溶解性和口服生物利用性. 最佳的药物辅助剂比率是成功开发利瓦洛克萨班配方的关键.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 制定 发展 制定 发展
背景情况:
- 里瓦罗克萨班 (RXB) 具有较差的水溶性,限制了其口服生物利用性.
- 开发有效的药物输送系统对于提高利瓦洛克萨班等溶性较差药物的治疗疗效至关重要.
研究的目的:
- 开发使用水溶性载体和表面活性剂的里瓦洛克萨班装载微球.
- 通过优化配方来改善里瓦洛克萨班的溶解性,溶解率和口服生物利用性.
主要方法:
- 使用聚乙烯 (PVP) K30 (PVP) 作为载体和硫酸 (SLS) 作为表面活性剂制备微球.
- 使用1H NMR和FTIR分析了药物辅助剂和辅助剂辅助剂相互作用.
- 对优化配方的溶解度,溶解率和口服生物可用性进行了评估.
主要成果:
- 优化的里瓦洛克萨班/PVP/SLS微球配方 (IV和VIII) 与里瓦洛克萨班粉末相比,分别增加了可溶性160倍和86倍.
- 120分钟的溶解速度在IV和VIII配方中提高了大约4.5和3.4倍.
- 口服生物利用率提高了2.4倍 (IV配方) 和1.7倍 (VIII配方),IV配方呈现出最高的增加 (AUC: 2400.8 ± 237.1h·ng/mL).
结论:
- 开发的微球有效地提高了里瓦洛克萨班的溶解性,溶解率和口服生物利用性.
- 里瓦洛克萨班,PVP和SLS之间的分子相互作用对于增强药物特性至关重要.
- 优化药物与辅助剂的比率对于使用这种方法成功开发里瓦洛克萨班配方至关重要.
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