作为Piribedil物理稳定性和生物可用性的调节器的水友和两友性大分子:对二进制混合物和状系统的研究
Luiza Orszulak1, Aldona Minecka2, Roksana Bernat3
1Institute of Chemistry, Faculty of Science and Technology, University of Silesia in Katowice, Szkolna 9, 40-006 Katowice, Poland.
本研究探讨了pribedil (PBD) 的聚合物矩阵,发现了一种新的PBD形式 (II). 星形PVP聚合物最能稳定无形PBD,而Soluplus菌根则提供卓越的长期稳定性和药物释放,提高生物可用性.
科学领域:
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
- 聚合物化学 聚合物化学
背景情况:
- 像皮里贝迪尔 (PBD) 这样的水溶性较差的药物存在配方挑战.
- 无形固体分散 (ASD) 和状系统是提高药物溶解性和生物可用性的策略.
- 无形活性药物成分 (API) 的物理稳定性对于有效的药物输送至关重要.
研究的目的:
- 调查不同拓和特性的聚合物作为皮里贝迪尔 (PBD) 的矩阵的使用.
- 评估聚合物类型和拓学对ASD和细胞系统中PBD物理稳定性,再结晶和药物释放的影响.
- 发现PBD的新多态形式并评估它们对配方性能的影响.
主要方法:
- 使用PBD与Soluplus,线性PVP (linPVP) 和星形PVP (starPVP) 制备无形固体分散 (ASD) 和状系统.
- 使用差分扫描热度计,X射线衍射,里埃变换红外光谱学和宽带介电光谱学进行表征.
- 评估物理稳定性,分子动力学,再结晶动力学和药物释放特征.
主要成果:
- 发现了一种新的多态形式 (II) 的皮里贝迪尔 (PBD).
- 含有水性PVP聚合物的ASD,特别是星形PVP (starPVP),证明了无形PBD的优越稳定性.
- 与PBD-starPVP ASD相比,使用Soluplus的状系统显示出最小的自组装尺寸分布和更高的长期稳定性.
- 所有测试的配方都改善了PBD的生物可用性,PBD-starPVP菌根表现出最有利的药物释放特征和最高的药物度.
结论:
- 聚合物的类型和结构显著影响无形药物的稳定及其释放特性.
- 星形PVP聚合物在稳定ASD无形PBD方面非常有效.
- 索鲁普卢斯是形成具有理想大小和长期稳定性的PBD菌根的最佳选择.
- 使用这些聚合物的新型PBD配方增强了药物的生物可用性,突出了药物设计中聚合物选择的重要性.
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