抗药克洛巴萨姆的无形状态:制备和表征
Marina M Marcos Valdez1, Julio Sanchez2, María E Bertotto3
1Facultad de Ciencias Químicas, Departamento de Ciencias Farmacéuticas y Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA)-Consejo Nacional de Investigaciones Científicas y Técnicas de la República Argentina (CONICET), Universidad Nacional de Córdoba, Ciudad Universitaria, Córdoba, X5000HUA, Argentina.
已经成功地制备和表征了无形的克洛巴萨姆 (CLOB). 然而,在各种压力条件下,这种无形形式很容易恢复到其晶体状态,这表明它没有明显的物理稳定性优势,而不是晶体CLOB.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 固态化学 固态化学
背景情况:
- 无形形式的药物可以提供更好的溶解性和生物可用性.
- 了解无形药物的物理稳定性对于配方开发至关重要.
- 克洛巴萨姆 (Clobazam,简称CLOB) 是一种抗药物,其固态特性对其治疗疗效很重要.
研究的目的:
- 准备和表征无形克洛巴萨姆 (CLOB-q).
- 在各种压力条件下调查无形CLOB的脱行为.
- 与其晶体形式 (CLOB-c) 相比,评估无形CLOB的物理稳定性.
主要方法:
- 用于制备无形CLOB的融灭技术.
- 使用显微镜 (PLM,HSM),X射线粉末衍射 (XRPD),DSC,DMA和XPS进行表征.
- 在温度/湿度,压缩和机械/热应力下进行脱研究.
主要成果:
- 无形CLOB (CLOB-q) 已成功准备并确认为真正的无形形式.
- CLOB-q的玻璃过渡温度 (Tg) 为67.0°C,被归类为脆弱的玻璃.
- 在各种压力条件下,包括高温/湿度和机械应力,CLOB-q完全脱玻璃化为晶体CLOB (CLOB-c).
结论:
- 无形CLOB首次合成并进行了表征.
- 无形的形式表现出不良的物理稳定性,容易在压力下结晶.
- 在物理稳定性方面,无形CLOB在晶体CLOB上没有明显的优势.
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