通过喷雾干燥的HPMC和基于香甘的固体分散物的洛素生物可用性工程:增强溶解性和治疗疗效
Sadia Pervez Lali1, Arooj Fatima1, Muhammad Sher1
1Institute of Chemistry, University of Sargodha Sargodha 40100 Pakistan msherawan@yahoo.com azhar.ramzan@uos.edu.pk +92 48-3768409 +92 300-6022454.
RSC advances
|January 30, 2026
概括
喷雾干燥使用聚合物制造了牛素 (OFL) 的固体分散物,显著提高了它在子中的溶解性和口服生物可用性. 这种配方增强了药物释放和治疗疗效.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 奥夫洛素 (OFL) 是一种诺类抗生素,其水溶性较差,限制了其口服生物利用性.
- 提高难溶药物的可溶性和溶解率对于改善治疗结果至关重要.
研究的目的:
- 通过使用固体分散 (SD) 技术来提高口服牛素 (OFL) 的生物可用性,溶解率和可溶性.
- 研究用水友性聚合物配制的喷雾干燥固体分散剂在增强药物输送方面的潜力.
主要方法:
- 使用基基甲基纤维素 (HPMC) 和香甘 (XNG) 作为载体进行喷雾干燥,制备了欧洛的固体分散剂 (SD).
- 描述涉及FT-IR光谱学,差分扫描热量计 (DSC),粉末X射线衍射 (PXRD) 和扫描电子显微镜 (SEM).
- 实验室药物释放研究是在模拟的胃条件下进行的,而体内药物动力学研究是在使用HPLC-UV方法在子身上进行的.
主要成果:
- FT-IR,DSC和PXRD证实了结合和晶体素在固体分散中转化为无形状态.
- SEM分析显示颗粒大小减少和表面形态变化,有助于提高溶解度.
- 在体外研究表明,与未经加工的OFL (59.2%) 相比,基于HPMC (97.88%) 和基于XNG (82.34%) 的SDs的药物释放显著增强.
- 与未经加工的OFL相比,对子的体内研究显示,SD配方的最大血度 (Cmax) 和延长半衰期 (t1/2) 显著增加,这表明其生物可用性有所提高.
结论:
- 使用HPMC和XNG的喷雾干燥固体分散物有效地提高了ofloxacin的可溶性,溶解率和体内性能.
- 这种配方策略有望提高水溶性较差的药物的治疗疗效,例如ofloxacin.
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