激光微干扰仪用于API可溶性和相位平衡:达鲁纳维尔作为一个案例
Veronika Makarova1, Mark Mandrik1,2, Sergey Antonov1
1A.V. Topchiev Institute of Petrochemical Synthesis, Russian Academy of Sciences, Leninsky pr. 29, 119991 Moscow, Russia.
Pharmaceutics
|July 30, 2025
概括
激光微干扰度准确地确定无形活性药物成分 (API) 的热力学可溶性和相位行为. 这种方法有助于选择辅助剂,并预测药物开发的配方稳定性.
科学领域:
- 制药科学 制药科学
- 物理化学 物理化学
- 材料科学 材料科学 材料科学
背景情况:
- 准确确定活性药物成分 (API) 溶解度和相位行为对于药物开发和稳定性至关重要.
- 传统的方法往往难以准确地确定相位过渡和可溶性极限,特别是对于不容易溶解的化合物.
研究的目的:
- 证明激光微干扰计在确定API的热力学可溶性方面的实用性.
- 将传统上用于聚合物系统的方法适应于制药应用.
主要方法:
- 激光微干涉度被用来测量无形达鲁纳维尔的热力学溶解度和相位行为.
- 实验在25-130°C的温度范围内,在各种药物溶剂中进行,包括油,水,甘油,酒精和糖醇.
- 溶解动力学和汉森溶解度参数也被评估用于比较分析.
主要成果:
- 达鲁纳维尔在瓦塞林和橄油中表现出实际的不溶性.
- 在水和糖醇中观察到具有上临界溶液温度的无形平衡,并构建了相位图.
- 在酒精,糖醇和乙氧化麻油衍生物中观察到高溶解度和晶体溶解物形成.
- 溶解速度差异很大,甲醇的溶解速度是乙醇的四倍,是异醇的三十倍.
- 实验数据和计算的可溶性参数之间发现了良好的相关性.
结论:
- 激光微干扰仪是确定API热力学溶解度和观察溶解过程的可行工具.
- 该方法可方便直接检测可溶性极限和相变,这对于配方开发至关重要.
- 这些发现支持明智地选择辅助剂,预防不必要的酸盐,并在早期药物开发中预测配方稳定性.
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