伊马替尼和姜黄素共晶混合物、共晶混合物和共晶混合物的比较研究:制备、表征和性能评价

IF 3.4 2区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
Hui-Tian Li, Xiao-Min Wang, Jin-Xia An, En Lin, Wei Li, Hai-Xin Qin, Jian-Feng Zhen, Xia-Lin Dai, Zhenjie Zhang, Tong-Bu Lu and Jia-Mei Chen*, 
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引用次数: 0

摘要

多药固体体系(共晶、共晶和共晶)提供了同时改善两种药物性能的潜力。然而,对于给定的药物组合,这些形式的系统比较仍然很少。伊马替尼(Imatinib, IM)和姜黄素(curcumin, CUR)具有协同抗癌活性,均属于BCS II类药物,溶解度和生物利用度较差。本文成功制备了含有IM和CUR的共晶混合物(IM-CUR EM)、共晶混合物(IM-CUR CM)和共晶混合物(IM-CUR CC),并对其进行了表征。综合DSC和PXRD分析表明,与单个组分相比,IM-CUR CC具有中等熔点和明显的衍射峰,而IM-CUR EM具有较低的熔化吸热,衍射模式不变。在PXRD分析中没有晶体反射(光晕模式),在DSC和调制DSC热图中都存在单个玻璃化转变事件,从而证实了IM-CUR CA的非晶化。晶体结构和红外光谱分析表明,IM的哌嗪N和CUR的酚O-H在共晶和共非晶相中都具有很强的分子间氢键。系统评价了其稳定性、溶解性和压实性以及抗癌活性。值得注意的是,IM-CUR EM具有更好的溶出性能,而IM-CUR CA和IM-CUR CC具有更好的抗癌效果。这三种固体形态均表现出优异的稳定性。比较研究为IM和CUR协同配方的开发提供了有价值的指导。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Comparative Investigation on a Eutectic Mixture, Coamorphous Mixture, and Cocrystal of Imatinib and Curcumin: Preparation, Characterization, and Property Evaluation

Comparative Investigation on a Eutectic Mixture, Coamorphous Mixture, and Cocrystal of Imatinib and Curcumin: Preparation, Characterization, and Property Evaluation

Multidrug solid systems (eutectic, coamorphous, and cocrystalline) offer potential to simultaneously improve both drugs’ properties. Yet, systematic comparisons of these forms for a given drug combination remain scarce. Imatinib (IM) and curcumin (CUR) demonstrate synergistic anticancer activity, and both are classified as BCS II drugs, characterized by poor solubility and bioavailability. Herein, a eutectic mixture (IM-CUR EM), coamorphous mixture (IM-CUR CM), and cocrystal (IM-CUR CC) involving IM and CUR were successfully prepared and fully characterized. Combined DSC and PXRD analyses revealed that IM-CUR CC exhibited an intermediate melting point and distinct diffraction peaks compared to individual components, whereas IM-CUR EM showed a lower melting endotherm with unchanged diffraction patterns. The amorphization of IM-CUR CA was verified by the absence of crystalline reflections (halo pattern) in the PXRD analysis and the presence of a single glass transition event in both DSC and modulated DSC thermograms. Crystal structure and FTIR analyses revealed strong intermolecular hydrogen bonding between the piperazine N of IM and phenolic O–H of CUR in both cocrystalline and coamorphous phases. Stability, dissolution and compaction performances, and anticancer activity were systematically evaluated. Notably, IM-CUR EM exhibited superior dissolution performance, while IM-CUR CA and IM-CUR CC showed an improved anticancer effect. All three solid forms exhibited excellent stability. The comparative study offers valuable guidance for the development of synergistic formulations of IM and CUR.

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来源期刊
Crystal Growth & Design
Crystal Growth & Design 化学-材料科学:综合
CiteScore
6.30
自引率
10.50%
发文量
650
审稿时长
1.9 months
期刊介绍: The aim of Crystal Growth & Design is to stimulate crossfertilization of knowledge among scientists and engineers working in the fields of crystal growth, crystal engineering, and the industrial application of crystalline materials. Crystal Growth & Design publishes theoretical and experimental studies of the physical, chemical, and biological phenomena and processes related to the design, growth, and application of crystalline materials. Synergistic approaches originating from different disciplines and technologies and integrating the fields of crystal growth, crystal engineering, intermolecular interactions, and industrial application are encouraged.
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