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开发Nebivolol口服片具有改善的溶解特性,基于其与环氧素的组合
Francesca Maestrelli1, Marzia Cirri1, Natascia Mennini1
1Department of Chemistry, School of Human Health Sciences, University of Florence, Via Ugo Schiff 6, 50019 Florence, Italy.
Pharmaceutics
|May 25, 2024
概括
使用硫乙-β-环极素 (SBEβCD) 的新型内比沃洛尔片显著改善了药物的溶解和生物可用性. 与参考片相比,囊配方提供更快的药物释放速度.
科学领域:
- 制药技术 制药技术 制药技术
- 药物输送系统 药物输送系统
- 物理药房 物理药房
背景情况:
- 尼比沃洛因溶解率和溶解率低而表现出较差的口服生物利用性.
- 循环德克斯复合是一种提高难溶性药物的可溶性的策略.
研究的目的:
- 开发新的口服内比沃片,使用循环德克斯特林复合剂改善溶解性和溶解性.
- 评估nebivolol-SBEβCD系统的固态和溶解特性,并与现有配方进行比较.
主要方法:
- 使用各种环氧化进行了相溶性研究,确定了硫乙烯-β-环氧化 (SBEβCD) 作为最佳药物.
- 通过共同蒸发来制备Nebivolol-SBEβCD固体分散物并进行了表征.
- 制定了药片和囊,并将其溶解概况与参考和商业产品进行了比较.
主要成果:
- 同蒸发的nebivolol-SBEβCD系统显示了增强的溶解速率和几乎完全的药物无形化.
- 开发的尼比沃洛尔片在60分钟内实现了100%的药物溶解,表现优于参考和商业片.
- 囊配方表现出快速释放药物,在20分钟内达到100%的溶解.
结论:
- 硫乙-β-环极素有效地增强了nebivolol用于口服的溶解特性.
- 尼比沃洛-SBEβCD片和囊代表了具有改善生物可用性潜力的先进配方.
- 可能需要进一步优化,以减轻SBEβCD对药片分解时间的影响.
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