基于trimethoprim的多组件固体系统:机械化学查,表征和抗菌活性评估
Giusi Piccirillo1, Rafael Aroso1, João A Baptista1
1University of Coimbra, Coimbra Chemistry Centre, Department of Chemistry, Rua Larga, 3004-535, Coimbra, Portugal.
International journal of pharmaceutics
|July 4, 2024
概括
机械化学创造了新的trimethoprim固体系统. 这些系统增强了trimethoprim.
科学领域:
- 制药科学 制药科学
- 固态化学 固态化学
- 药用化学 医学化学
背景情况:
- 三甲 (TMP) 是一种重要的抗生素,其可溶性和活性有限.
- 开发新的配方可以提高药物的疗效和患者的治疗结果.
- 机械化学提供了一种无溶剂的方法,用于制造先进的医药固体.
研究的目的:
- 开发使用机械化学的三甲 (TMP) 多组件固体系统.
- 通过辅助器选择来增强TMP的水溶性,溶解率和抗菌活性.
- 为了识别具有改善药物性能的TMP的新型盐和优混合物.
主要方法:
- 二元和等分系统的机械化学合成,使用GRAS辅构剂和其他API.
- 使用热分析,粉末X射线衍射 (PXRD) 和富里埃变换红外光谱法 (FTIR) 进行了表征.
- 评估内在溶解速率和抗菌活性对抗阳性和阴性细菌.
主要成果:
- 确定了3个等分系统作为盐和4个作为优菌混合物.
- 通过尼古丁酸 (盐) 提高了TMP溶解率25%,通过降醇 (舒缓剂) 提高了5%.
- 观察到几个TMP-coformer系统的增强抗菌活性,特别是针对E. coli与黄素和西普罗夫洛克萨.
结论:
- 机械化学制备的多组件TMP系统提供了更好的溶解速率和增强的抗菌疗效.
- 配合剂的选择对于优化TMP的药物和抗菌特性至关重要.
- 这些发现为传统的三甲胺配方提供了一个有希望的替代品.
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