具有不同表面微观结构的新型里瓦洛克萨班装载微球系统,可增强口服生物利用性
Min-Jong Choi1, Mi Ran Woo2, Kyungho Baek1
1Department of Pharmaceutical Engineering, Dankook University, 119 Dandae-Ro, Dongnam-Gu, Cheonan, 31116, South Korea.
Drug delivery and translational research
|September 4, 2023
概括
这项研究开发了三种类型的Rivaroxaban装载的聚合物微球. 溶剂蒸发的微球显著增强了里瓦洛克萨班.
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:
- 里瓦罗克萨班是一种广泛使用的抗凝剂,具有较差的水溶性,限制了其口服生物可用性.
- 开发有效的药物输送系统对于提高像利瓦洛克萨班这样的溶性较差药物的治疗疗效至关重要.
研究的目的:
- 制造和比较具有不同表面微观结构的三种类型的里瓦洛克萨班装载聚合物微球.
- 为了评估这些微球对利瓦洛克萨班的可溶性,溶解率和口服生物利用性的影响.
主要方法:
- 使用喷雾干燥技术 (溶剂蒸发,表面附着,溶剂湿) 制造里瓦洛克萨班装载的聚合物微球.
- 使用SEM,XRD,DSC和粒子大小分析对微球物理化学性质的表征.
- 在体外评估水溶性和溶解速度,然后在体内评估大鼠口服生物可用性.
主要成果:
- 溶剂蒸发的微球呈现出明显更高的水溶性 (约. 208x) 和溶解率 (大约. 5x) 与里瓦洛克萨班粉末相比.
- 这三种类型的微球都改善了里瓦洛克萨班的口服生物可用性,溶剂蒸发的微球显示出最大的增加 (约. 2x) 的意思.
- 口服生物利用度的改善顺序是:溶剂蒸发 > 溶剂湿 > 表面附着的微球.
结论:
- 用溶剂蒸发的里瓦罗克萨班装载的聚合物微球代表了一种有前途的新型口服剂型.
- 这种配方策略有效地提高了口服难溶性里瓦洛克萨班的生物可用性.
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