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通过喷雾干燥制备的阿托瓦斯塔丁三水合物与同形普罗布科尔的改善溶解特性
Shinji Oyama1, Noriko Ogawa1, Kaori Kawai1
1Department of Pharmaceutical Engineering, School of Pharmacy, Aichi Gakuin University.
Chemical & pharmaceutical bulletin
|February 18, 2024
概括
喷雾干燥普鲁科尔 (PC) 和阿托瓦斯塔丁 (ATO) 创造了一个共形系统,显著改善了PC.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 普罗布科尔 (PC) 具有较低的水溶性,限制了其治疗功效.
- 阿托瓦斯塔丁三水酸盐 (ATO) 作为一种增强药物特性的辅助形成剂.
- 喷雾干燥是一种用于无形固体分散配方的常见技术.
研究的目的:
- 通过喷雾干燥,准备一个共形系统的普鲁科尔 (PC) 和阿托瓦斯塔丁 (ATO).
- 描述同形态系统的物理化学特性和稳定性.
- 为了评估同形变化的影响,probucol.的溶解速度.
主要方法:
- 喷雾干燥 (SD) 用于准备PC和ATO的共同形态系统.
- 物理化学表征包括粉末X射线衍射 (PXRD),热分析和FTIR.
- 在加速条件下 (40°C/75%RH) 进行了溶解试验和稳定性研究.
主要成果:
- 通过PXRD和热分析证实了通过SD形成PC-ATO共形系统.
- 与晶体PC或物理混合物相比,共形系统显示了PC的增强溶解概况.
- 同形态材料表现出优越的稳定性,在35天内保持无形,与无形PC不同,该材料在一天内结晶.
结论:
- 喷雾干燥成功地产生了一个稳定的probucol和atorvastatin的共同形态系统.
- 同形态化显著提高了水溶性和溶解率的probucol.
- 这种方法提供了一种可行的策略,可以提高像普鲁科尔这样溶解不良药物的生物可用性.
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