水友性聚合物对利瓦罗克萨班/β-环氧德克斯综合物的可溶性和溶解增强的影响
Waqas Haider Khan1, Sajid Asghar1, Ikram Ullah Khan1
1Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, 38000, Pakistan.
Heliyon
|October 9, 2023
概括
这项研究使用β-cyclodextrin (βCD) 和性聚合物增强了疏水性药物里瓦罗克萨班的溶解性和溶解性. 三级包容复合物,特别是Soluplus (SOLO),显示出最显著的改善.
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:
- BCS II类药物如利瓦洛克萨班具有较差的水溶性,导致吸收不稳定.
- 提高溶解度和溶解度对于改善这种疏水性药物的生物可用性至关重要.
研究的目的:
- 为了研究β-cyclodextrin (βCD) 和水性聚合物 (poloxamer 188,聚乙烯 pyrrolidone,Soluplus) 对里瓦罗克萨班的溶解性和溶解的影响.
- 开发和描述二元和三元包容复合体,以改善药物输送.
主要方法:
- 使用和溶剂蒸发制备与βCD的里瓦罗克萨班的二元包容复合物.
- 用优化的二进制系统和水友性聚合物制造三元包容复合物.
- 评估和溶解度和溶解概况.
- 使用FTIR,DSC,XRD和SEM进行固态表征.
主要成果:
- 里瓦洛克萨班的二元复合物:βCD (1: 2摩尔比) 与纯里瓦洛克萨班相比显示出增强的溶解性和药物释放性.
- 三级包容复合物进一步提高了溶解性和溶解性,其中 (1:2 药物:βCD:Soluplus 10% S.E) 配方表现出最大的增强.
- 固态分析证实了纳入复合物的形成和改进性质.
结论:
- 三次性纳入复合比二次性复合更有效地增强水性药物的可溶性和溶解性,如利瓦洛克萨班.
- 与βCD结合使用的Soluplus显著改善了里瓦洛克萨班的溶解特征.
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