药物-脂共形配方:制备方法和脂选择的作用
Keyoomars Khorami1, Sam Darestani Farahani1, Anette Müllertz1
1Department of Pharmacy, Faculty of Health and Medical Science, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Pharmaceutics
|January 8, 2025
概括
共同形态脂系统 (CAPS) 用溶剂蒸发方法成功制备了多种难溶药物. 这些系统表明药物的溶解和稳定性得到了增强,特别是在1.5:1的药物与脂比率下.
科学领域:
- 材料科学 材料科学 材料科学
- 制药技术 制药技术 制药技术
- 药物输送系统 药物输送系统
背景情况:
- 水溶性较差的药物在制药配方中带来了挑战.
- 同形脂系统 (CAPS) 提供了一种有前途的方法来提高药物的溶解性和生物可用性.
- 有限的知识存在于CAPS的形成和稳定性与各种各样的药物和脂.
研究的目的:
- 探索与赛莱科克西布,罗塞米德,尼洛丁尼和利托纳维尔一起形成共形脂系统 (CAPS).
- 调查不同制备方法 (球磨,冷却冷却,溶剂蒸发) 对CAPS形成和稳定性的影响.
- 评估已开发的CAPS的溶解行为和物理稳定性.
主要方法:
- 共同形态脂系统 (CAPS) 使用球磨 (BM),冷却冷却 (QC) 和溶剂蒸发 (SE) 方法进行制备.
- 首先选了等等分子药物与脂 (PL) 的比率,然后对各种分子比率 (例如1.5:1) 和过量的PL进行了调查.
- 固态特征包括X射线粉碎衍射 (XRPD),极化光显微镜 (PLM) 和微分扫描热量计 (DSC);物理稳定性被评估为0%和75%的RH.
主要成果:
- 溶剂蒸发 (SE) 是最一致的方法,以准备CAPSs与赛莱科西布 (CCX),罗西米德 (FUR),和利托纳维尔 (RIT).
- 对CCX和RIT来说,CAPS表现出增强的溶解,脂提供轻微的沉抑制.
- 在SE准备的CAPS中,物理稳定性得到了显著的改善,特别是在1.5:1的摩尔比率或过多的PL时.
结论:
- 共同形态脂系统 (CAPS) 可以使用溶剂蒸发方法有效地制备,支持它们在选过程中的使用.
- 与传统的药物聚合物系统相比,这些系统允许相对较高的药物负载.
- 药物选择,制备方法和脂类型是开发稳定有效的CAPS的关键因素.
关键词:
变形无形化是一种无形化过程.球磨机 球磨机 球磨机同形态系统是共形态系统.溶解增强增强方法 溶解增强方法药物的稳定性 药物的稳定性脂质是一种脂质.水溶性较差的药物 在水溶性较差的药物灭冷却的冷却方式固态特征的固态表征溶剂的蒸发是溶剂的蒸发.更多相关视频
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