评估药物物质颗粒大小的新技术在复杂的吸入配方中
Daniel P Dobson1, Miguel Saggu1, Jackson D Pellett1
1Genentech, 1 DNA Way, South San Francisco, CA 94080, United States.
Journal of pharmaceutical sciences
|July 8, 2023
概括
本研究提出了一种新的激光衍射方法,用于测量干粉吸入器中活性药物成分 (API) 颗粒大小稳定性. 较低的药物负载提高了API粒子的稳定性,这可能是由于凝聚性相互作用减少.
科学领域:
- 制药技术 制药技术 制药技术
- 粒子科学 粒子科学
- 药物输送系统 药物输送系统
背景情况:
- 干粉吸入器 (DPI) 使用活性药物成分 (API) 和载体辅助物质进行肺部药物输送.
- 在DPI配方中保持API颗粒大小稳定性对于一致的空气动力学性能至关重要.
- 测量API粒子大小是具有挑战性的,因为在标准激光衍射中,高辅助剂度会掩盖API信号.
研究的目的:
- 开发一种新的激光衍射方法,用于准确测量DPI中的API粒子大小稳定性.
- 调查药物负载对DPI配方中的API颗粒大小稳定性的影响.
- 了解药物负载,凝聚性相互作用和颗粒大小稳定性之间的关系.
主要方法:
- 开发了一种新的激光衍射技术,利用API和助剂之间的溶解度差异.
- 该方法用于分析DPI混合物中各种药物加载度的API颗粒大小稳定性.
- 配方混合物的特征是为了评估药物加载效应和潜在的凝聚性相互作用.
主要成果:
- 这种新的方法成功测量了API颗粒大小稳定性,克服了高辅助剂水平带来的挑战.
- 与高药载荷配方相比,低药载荷配方显示出明显更好的API颗粒大小稳定性.
- 在较低的药物负载配方中减少的凝聚性相互作用被认为是改善颗粒大小稳定的原因.
结论:
- 开发的激光衍射方法为DPI中的API粒子稳定性提供了宝贵的见解.
- 药物负载是影响API粒子大小稳定的关键因素,较低的负载更稳定.
- 了解这些稳定性动态对于优化DPI配方设计和确保有效的肺药物递送至关重要.
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