新型共形西洛斯塔的物理特性;制备方法和摩尔比对共形西洛斯塔的影响
Tomoki Takayama1, Shun Kaneko2, Vasanthi Palanisamy1
1Department of Molecular Pharmaceutics, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose, Tokyo 204-8588, Japan.
Chemical & pharmaceutical bulletin
|April 2, 2025
概括
本研究探讨了cilostazol-l-tryptophan共同形态系统的不同比例和制备方法如何影响药物特性. 最佳的比率和方法显著提高了难溶性药物的溶解性和稳定性.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 同形态系统增强了难溶性药物的口服生物可用性.
- 有限的研究存在于药物活性成分 (API) 对同形前 (CF) 摩尔比和制备方法对同形性质的影响.
研究的目的:
- 为了研究摩尔比率和制备方法对新型西洛斯塔-l-托共形系统的物理性质的影响.
- 评估准备的共形系统的分子状态和稳定性.
主要方法:
- 基洛斯塔和l-氨酸的共同形态系统是使用1: 1,1: 1.5和1: 2摩尔比率的共同研磨 (CM) 和1: 1摩尔比率的喷雾干燥 (SD) 制备的.
- 评估了溶解度,储存稳定性和分子状态 (使用固态13C-NMR).
主要成果:
- 1:1.5和1:2 (CM 1:1.5,CM 1:2) 的共同研磨比率表现出最高的溶解度.
- 观察到CM 1:1.5,CM 1:2,SD 1:1的存储稳定性非常好.
- 同变形改善了物理性能,有证据表明西洛斯塔和l-三之间存在键.
- 固态13C-NMR显示了共磨和喷雾干燥样品之间的分子状态的差异.
结论:
- API与CF的摩尔比率和制备方法显著影响着cilostazol-l-tryptophan共同形态系统的物理性质和分子状态.
- 同形化是一种可行的策略,可以提高基洛斯塔的可溶性和稳定性.
- 根据制备方法对特定分子相互作用进行进一步的研究是有必要的.
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