罗苏瓦斯塔丁加载固体纳米分散剂的配方和评估,以提高其可溶性
Selvakumar Muruganantham1, Venkateshwaran Krishnaswami2, Cathrien Joseph1
1Department of Pharmaceutics, Vivekanandha Pharmacy College for Women, Sankari, 637303 Salem, Tamil Nadu, India.
Annales pharmaceutiques francaises
|November 29, 2025
概括
这项研究开发了罗苏瓦斯塔丁载固体纳米分散剂 (RcNDs),以提高可溶性和口服生物可用性,用于高胆固醇血症治疗. 优化的RcNDs-4配方显著改善了药物释放和溶解度,解决了传统口服药物的局限性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术纳米技术
背景情况:
- 罗斯瓦斯塔丁是一种治疗高胆固醇血清症的强效他类药物,但由于溶解度低和第一通代谢,其口服生物可用性较差.
- 提高罗斯瓦斯塔丁的可溶性和生物利用性对于有效的HMG-CoA减少酶抑制和治疗至关重要.
研究的目的:
- 开发和描述罗苏瓦斯塔丁载固体纳米分散剂 (RcNDs),以提高罗苏瓦斯塔丁的溶解性和治疗疗效.
- 研究纳米分散配方在改善难溶药物的口服药物输送方面的潜力.
主要方法:
- 固体纳米分散剂 (RcNDs) 使用溶剂蒸发技术与聚乙烯基罗利丁K30和Poloxamer407.7一起制备.
- 对配方的物理化学特性进行了评估,包括粒子大小,泽塔潜力,药物含量,捕获效率和体外药物释放.
主要成果:
- 优化的RcNDs-4配方表现出有利的特性:粒子大小 (193.27±6.35nm),泽塔电位 (-8.72±0.23mV),药物含量 (9.14±0.18mg) 和捕获效率 (90.894±3.50%).
- 与纯罗斯瓦斯塔丁相比,RcNDs-4的药物释放概况 (93.49±1.52%) 显著更高.
- 形态和热分析表明药物嵌入纳米分散和无形状态,有助于提高溶解度.
结论:
- 开发的纳米扩散配方有效地改善了罗斯瓦斯塔丁的溶解性和溶解性.
- 纳米分散技术提供了一种有前途的方法,可以提高口服生物可用性,并减少BCSII类药物的副作用,如罗斯瓦斯塔丁.
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