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泰尔米沙坦的多元组件无形固体形式:对机械化学激活和物理化学属性的洞察

Jamshed Haneef¹, Shakir Ali²

¹Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, 110062, India. jamshedhaneef@jamiahamdard.ac.in.

AAPS PharmSciTech

|April 11, 2024

概括

机械化学合成创造了新型无形固体形式的telmisartan (TEL) 与α-甲酸 (KGA) 和谷氨酸 (GA). 这些形式显著增强了TEL.

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:

泰尔米沙坦 (TEL) 是一种血管激素II受体阻塞剂,具有较差的物理化学性质.
开发新的固体形式对于提高药物的溶解性和生物可用性至关重要.
机械化学为固态药物配方提供了一种溶剂最小化的方法.

研究的目的:

探索使用α-谷氨酸 (KGA) 和谷氨酸 (GA) 作为辅助剂的特尔米沙坦 (TEL) 新型固体形式.
研究机械化学制备的固体形式在增强物理化学参数中的作用.
了解无形介导共结晶的机制.

主要方法:

机械化学合成使用TEL和与催化乙醇共成型剂的1:1稳定度比.
通过粉末X射线衍射 (PXRD),差分扫描热度计 (DSC) 和富里埃变形红外光谱 (FTIR) 进行表征.
对表面可溶性,内在溶解和物理稳定性的评估;用于表面分析的FESEM和EDX映射.

主要成果:

机械化学合成的结果是通过无形介导的共结晶形成无形固体形式 (TEL-KGA和TEL-GA).
与纯TEL.相比,明显可溶性 (8-10倍) 和内在溶解释放 (6-9倍) 的显著增加.
证明了无形介导的共结晶,涉及分子识别,中间无形阶段和产物核化.

结论:

通过机械化学制备的无形相对于通过无形介导的共晶化进行共晶研究具有前景.
这些无形形式在可溶性和溶解动力学上提供了实质性的改进.
转移稳定的共晶相可以防止快速降水,增强整体物理化学性质.

关键词:

无形固体形式是无形的固体形式.协同晶体协同晶体是一个晶体工程是什么意思水晶工程机械化学合成机械化学合成弹 - 降落效应

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