通过使用计算和实验方法,通过冷解固体分散增强赛莱可西布的可溶性
Fatima Rasool1, Ayesha Naseem2, Huma Javaid2,3
1Punjab University College of Pharmacy, Faculty of Pharmacy, University of the Punjab, Lahore, 54590, Pakistan. fatima.pharmacy@pu.edu.pk.
Scientific reports
|October 21, 2025
概括
这项研究提高了使用基烯基β-环氧化 (HP-βCD) 固体分散的赛莱科西布 (CLX) 溶解性和溶解性. 优化的HP-βCD系统显著改善了CLX口服生物可用性.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 计算化学计算化学
背景情况:
- 切莱可西布 (CLX) 是一种选择性COX-2抑制剂,具有较差的水溶性和溶解性,限制了其口服生物利用性.
- 它的BCSII类分类要求制定策略来改善治疗骨关节炎和类风湿性关节炎等疾病的药物输送.
研究的目的:
- 通过集成的计算和实验方法来增强赛莱科西布 (CLX) 的溶解性和溶解性.
- 开发一种有效的药物递送系统,以改善CLX口服生物可用性.
主要方法:
- 计算模拟 (晶体形态学,分子动力学) 确定了基乙-环极 (HP-βCD) 作为一种兼容的聚合物.
- 准备和表征了CLX-HP-βCD的冷化固体分散物 (SD).
- 进行了体外溶解测试和成片的配方.
主要成果:
- 惠普-βCD显示了与CLX的有利相互作用参数 (χ = -5.86,Emix = -3.47 kcal/mol).
- 软化固体分散SD1实现了可溶性增加150倍 (645微克/毫升),并增强了溶解.
- 从SD1制成的片 (T1) 在3小时内几乎完全释放药物 (99.88%).
结论:
- 基于HP-βCD的冷解固体分散是一种高度有效的系统,可以增强赛莱可克西布的溶解性和溶解性.
- 这种方法显著改善了 celecoxib 的口服生物可用性.
- 开发的固体分散技术有望改善难溶性药物的输送.
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