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基于实验和模型的方法来评估溶剂对药物artemisinin溶解度的影响
Steffi Wünsche1, Vico Tenberg1, Karina Oliynyk1
1Max Planck Institute for Dynamics of Complex Technical Systems, Magdeburg, Germany.
概括
使用n-heptane进行抗溶剂结晶,有效地从植物提取物中净化了抗疟疾的美术素 (ARTE). 像Jouyban-Acree这样的预测模型准确地预测溶解度,减少了制药开发中的实验需求.
科学领域:
- 制药工艺开发 制药工艺开发
- 化学工程是化学工程的重要组成部分.
- 药用化学 医学化学
背景情况:
- 植物性活性药物成分 (API) 的净化至关重要.
- 抗溶剂结晶是净化诸如甲美西宁 (ARTE) 等化合物的关键技术.
- 阿尔特梅西亚年菜L.的托卢烯提取物含有艺术素.
研究的目的:
- 为了评估用于美素净化的抗溶剂结晶.
- 为了确定artemisinin在烯/n-heptane和烯/乙醇混合物中的可溶性.
- 在二元溶剂系统中确定可溶性的预测模型.
主要方法:
- 在温度范围 (278.15 K至313.15 K) 中,对二元溶剂混合物 (托卢/n-赫,托卢/乙醇) 中的素溶解度的实验性确定.
- 应用和比较PC-SAFT模型 (带有和没有配合的二进制相互作用参数) 和Jouyban-Acree模型.
- 在预测溶解度和区分有效抗溶剂方面评估模型准确性.
主要成果:
- 证明N-heptane是一种有效的抗溶剂,而乙醇则作为辅溶剂.
- 所有测试的模型都能区分有效和无效的抗溶剂.
- 朱伊班-阿克里模型在匹配实验数据方面表现出最高的准确性,需要至少十个数据点进行参数化.
- 配合二元相互作用参数的PC-SAFT模型 (kij) 显示出比纯预测版本 (kij = 0) 更好的准确性.
结论:
- 使用n-heptane进行抗溶剂结晶是一种可行的素净化方法.
- 预测性溶解度模型显著减少了用于制药开发的溶剂选中的实验力度.
- 在这种情况下,与PC-SAFT相比,Jouyban-Acree模型在二元溶剂混合物中的可溶性预测中提供了更高的准确性.
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