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从机械化学驱动的复杂性和多模式特性到稳定性和毒理学洞察力:对辛纳瑞-β-环极素复杂物的研究

David Klarić¹, Lucija Kutleša¹, Mario Jug²

¹Department of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, 10 000 Zagreb, Croatia.

|October 29, 2025

概括

通过机械激活与环极素 (CDs) 复合的辛纳利津 (CIN) 显著改善了药物的溶解. 由此产生的肉素/环素复合物显示出新药配方的前景,而不会影响稳定性.

科学领域:

制药科学制药科学
药物输送系统药物输送系统
材料科学材料科学材料科学

背景情况:

辛纳瑞 (CIN) 具有较差的溶解性,限制了其用于前体疾病的治疗用途.
已知循环二烯 (CDs),包括β-循环二烯 (βCD),基二烯-β-循环二烯 (HPβCD) 和硫二烯-β-循环二烯 (SBEβCD),可增强药物溶解性.
机械激活提供了一种无溶剂的方法,用于制备药物-环德林复合物.

研究的目的:

通过机械激活来制备和表征1:1的肉素/环素复合物.
评估环德克斯复合对锡纳瑞溶解速率和稳定性的影响.
开发和验证一种稳定性指示方法,用于分析辛纳及其潜在的降解产物.

主要方法:

使用高能振动磨粉,用βCD,HPβCD和SBEβCD复合利.
通过差分扫描热量测量 (DSC),热重力测量分析 (TGA),X射线粉末衍射 (XRPD) 和福里埃转换红外 (FTIR) 光谱学进行固态特征化.
在酸盐缓冲体 (pH4.5) 中溶解研究,在各种条件下的稳定性评估,以及UHPLC-DAD-HRMS分析以量化和降解产品识别.

主要成果:

固态分析证实了地面产品中成功的肉素-环素相互作用.
辛纳/HPβCD复合体表现出最高的溶解效率.
在加速稳定条件下没有检测到任何降解产品,这表明复合物的化学稳定性很好.

结论:

锡纳利与循环德克斯特林的固态复合有效地增强了药物的溶解.
准备好的肉素/环素复合物表现出良好的稳定性,使其适用于新型药物配方.
机械激活是一种可行的技术,用于生产稳定和改进的辛纳瑞药物递送系统.

关键词:

化学稳定性化学稳定性辛纳里辛 (cinnarizine) 是一种一种循环德克斯特林 (cyclodextrins) 是一个循环德克斯特林.降解剂降解剂是一种降解剂.在体外溶解溶解.在体外的透性.机械化学机械化学固态特征的固态特征表征毒性的毒性毒性的毒性

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