准备,表征和在体外评估阿托瓦斯塔丁纳米悬浮
Yaman Ahmad Akour1, Ahmad Aljaberi1, Saja H Hamed2
1Department of Pharmaceutical Sciences and Pharmaceutics, Faculty of Pharmacy, Applied Science Private University, Amman, Jordan.
PloS one
|October 21, 2025
概括
这项研究开发了一种冷化阿托瓦斯塔丁纳米悬浮剂,以改善药物溶解. 优化的纳米悬浮在酸性介质中显示出增强的溶解,显示出难溶性药物的潜力.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 纳米技术 纳米技术
背景情况:
- 水溶性较差的药物在口服药物开发中存在挑战,原因是溶解有限和药物动力学变化.
- 阿托瓦斯塔丁是一种广泛使用的降胆固醇药物,具有较低的水溶性,需要制定策略来提高其生物可用性.
研究的目的:
- 使用纳米悬浮技术增强阿托瓦斯塔丁的溶解和生物可用性.
- 准备和表征解冷化阿托瓦斯塔丁纳米悬浮剂与优化的配方.
主要方法:
- 阿托瓦斯塔丁纳米悬浮剂是使用抗溶剂技术与各种稳定剂制备的.
- 纳米悬浮被使用曼尼托尔或三糖作为冷保护剂解.
- 特性包括粒子大小,泽塔潜力,PDI,DSC,XRD,FTIR和体外药物释放研究.
主要成果:
- 使用2%的多F127和80毫克曼尼托尔的优化配方在溶解后获得了54.5nm的平均颗粒大小,zeta潜力为-0.809,PDI为0.141.
- 在冷化纳米悬浮剂中,XRD和DSC表明阿托瓦斯塔丁的部分无形化.
- FTIR证实了阿托瓦斯塔丁与辅助剂之间的物理相互作用,聚合物和溶解保护剂可保存药物纳米颗粒.
- 与创新产品Lipitor®相比,冷化纳米悬浮在0.1N HCl中显示出更好的溶解.
结论:
- 取得了稳定,冷化阿托瓦斯塔丁纳米悬浮剂的成功制备.
- 助剂选择对于纳米悬浮的稳定性,固态特性和药物释放至关重要.
- 开发的纳米悬浮配方有望改善托瓦斯酸等水溶性较差的药物的输送.
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