固态选和干粉吸入器开发的ziyuglycoside II盐提高生物可用性
Hanwen Zhang1, Siwen Wang2, Sara Slimani2
1College of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China; Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201210, China.
International journal of pharmaceutics
|June 18, 2025
概括
齐尤格利科西德II (ZYG II) 由于溶解性差,其生物利用性较低. 开发ZYG II盐 (ZYG-II-Na) 干粉吸入器显著改善了其吸收和生物可用性.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 来自Sanguisorba officinalis L.的沙波宁Ziyuglycoside II (ZYG II) 具有有限的药理作用,原因是其口服生物利用率低 (<5%),由于溶解性低,透性低,以及广泛的第一通代谢.
- 提高ZYG II的生物可用性对于其治疗应用至关重要.
研究的目的:
- 为了提高zyuglycoside II (ZYG II) 的可溶性和口服生物利用性.
- 开发和描述ZYG II盐 (ZYG-II-Na) 的固体形式,并制定干粉吸入器 (DPI) 进行增强的肺部输送.
主要方法:
- 使用结构分析,稳定性评估和粉末评估,对ZYG-II-Na固体形式 (晶体和无形) 的系统选和表征.
- 在小鼠体内溶解性研究和体内药理动力学评估.
- ZYG-II-Na DPI的配方和空气动力学评估.
主要成果:
- 确定了三种晶体 (I,II,III) 和两种无形 (I,II) 的ZYG-II-Na形式,其中无形I和II表现出增强的可溶性稳定性.
- 与其他形式相比,水晶III表现出优越的湿度稳定性.
- 与口服 (3.53%) 相比,ZYG-II-Na DPI在老鼠中使用导致生物可用性显著增加 (水晶I的8.54%,无形II的16.8%).
结论:
- 固体形式优化和DPI配方有效地克服了ZYG II的生物可用性限制.
- 通过DPI输送的无形ZYG-II-Na提供了一种有前途的策略,可以提高这种沙素的治疗效果.
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