不同离心参数对平衡溶解度测量的不同离心参数的影响
Rita Szolláth1,2, Vivien Bárdos1,2, Marcell Stifter-Mursits1,2
1Department of Pharmaceutical Chemistry, Semmelweis University, Hőgyes E. u. 9., H-1092 Budapest, Hungary.
Methods and protocols
|October 28, 2025
概括
在和摇动瓶法中优化离心,对于准确的药物溶解度确定至关重要. 预沉积和较短,较慢的离心旋转为药物生物可用性研究提供了更可靠的结果.
科学领域:
- 制药科学 制药科学
- 药物开发 药物开发
- 物理化学 物理化学
背景情况:
- 药物的生物可用性与溶解性密切相关,在药物开发过程中需要早期和准确的确定.
- 和振动瓶 (SSF) 方法是溶解度测量的标准,相位分离是关键步骤.
- 阶段分离技术,特别是离心法,可以显著影响溶解度测量的准确性.
研究的目的:
- 用SSF方法研究离心参数 (时间和速度) 对药物溶解度测量的影响.
- 为了比较不同样品制备方案 (连续和后沉) 对溶解度结果的影响.
- 为了确定最佳的离心条件,以可靠和准确地确定溶解度.
主要方法:
- 四个模型化合物在三个pH值下使用布里顿-罗宾逊缓冲器进行了测试.
- 使用和振动瓶 (SSF) 方法测量溶解度.
- 离心术以不同的速度 (5000或10,000rpm) 和持续时间 (5,10或20分钟) 进行.
- 两种样品制备方法进行了比较:24小时的连续和6小时的,然后在离心前进行18小时的沉积.
主要成果:
- 在离心之前对样品进行预沉积,导致溶解度值接近仅沉积的参考值.
- 连续方案往往导致过高的溶解度值,特别是在更高的速度和更长的离心时间.
- 在没有预沉积的情况下进行长时间的高速离心后,帕帕维林化的溶解度值提高了60-70%.
- 较短,较慢的离心 (5分钟在5000rpm) 显示较低的标准偏差和结果最接近参考值.
结论:
- 离心参数和样品制备方法显著影响药物溶解度的测量.
- 建议进行预沉积,以提高通过离心机获得的可溶性数据的准确性.
- 优化,更温和的离心条件 (更短的时间,更低的速度) 对于在早期药物开发中可靠地确定药物溶解度至关重要.
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