在某些有机溶剂中对皮拉津胺溶解过程的热力学评估
Jesus Tovar-Amézquita1, Cristian Rincón-Guio2, Francy Elaine Torres-Suarez3
1Sitafi Group Ingeniería S.A.A., Palermo 412001, Huila, Colombia.
Molecules (Basel, Switzerland)
|November 9, 2024
概括
这项研究研究了pyrazinamide在九种有机溶剂中的溶解性. 最大溶解度发生在二甲基硫氧化物中,由驱动,对结核病药物开发至关重要.
科学领域:
- 制药科学 制药科学
- 物理化学 物理化学
- 药用化学 医学化学
背景情况:
- 结核病仍然是全球主要的健康问题,在2022年导致超过130万人的死亡.
- 皮拉津胺是关键的第一线结核病治疗,突出其药物重要性.
- 溶解度是影响药物配方和疗效的关键物理化学性质.
研究的目的:
- 在九种具有药学意义的有机溶剂中进行皮拉津胺的热力学可溶性研究.
- 为了确定温度对不同溶剂中皮拉津胺胺溶解度的影响.
- 为了计算pyrazinamide的热力学参数和可溶性参数.
主要方法:
- 使用摇动瓶法来确定溶解度.
- 采用紫外线/Vis光谱光度测量技术进行pyrazinamide的定量分析.
- 在9个温度 (283.15 K到318.15 K) 中测量了溶解度.
主要成果:
- 皮拉津胺在二甲基硫氧化物中具有最大可溶性 (x2=0.0816±0.004在318.15 K) 和在环素中具有最小可溶性 (1.73±0.05×10-5在283.15 K).
- 热力学分析揭示了一个内热溶解过程,其中是主要的驱动因素.
- 使用Hoftyzer-van Krevelen (32.90 MPa^1/2) 和Bustamante (28.14 MPa^1/2) 方法计算的可溶性参数.
结论:
- 实验性溶解度数据对于理解pyrazinamide在各种溶剂中的行为至关重要.
- 热力学概况表明驱动的溶解,这对于配方设计很重要.
- 调查结果为优化pyrazinamide药物形式和药物输送系统提供了必要的数据.
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