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利古斯特拉的新型共晶:增强高度和稳定性

Yifei Xie¹, Lixiang Gong², Yue Tao²

¹Beijing City Key Laboratory of Drug Target and Screening Research, National Center for Pharmaceutical Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.

Molecules (Basel, Switzerland)

|May 25, 2024

概括

晶技术增强了Ligustrazine (TMP) 的稳定性,这是Rhizoma Chuanxiong中的活性化合物,用于心血管疾病. 新型共晶体显著降低了吸收水分,并提高了热稳定性.

科学领域:

制药科学制药科学
材料科学材料科学材料科学
化学工程是化学工程的重要组成部分.

背景情况:

来自Rhizoma Chuanxiong的ligustrazine (TMP) 对于治疗心血管和脑血管疾病至关重要.
TMP的临床实用性受到其固有的不稳定性和升华倾向的限制.
晶技术提供了一个有前途的策略,以提高药品活性成分的物理化学稳定性.

研究的目的:

研究共晶形成在改善利古斯特拉辛 (TMP) 稳定性的潜力.
为了合成和描述新型的TMP共晶与精选的酸衍生物.
评估共结晶对TMP高度和热性质的影响.

主要方法:

利古斯特拉 (TMP) 与P-氨基酸 (PABA),3-氨基酸 (MABA) 和3,5-丁酸 (DNBA) 的联合结晶.
共同晶体形成的表征和静态测量 (TMP-PABA (1:2),TMP-MABA (1.5:1),TMP-DNBA (0.5:1)). 在这种情况下,晶体形成的特征是:
使用动态蒸汽吸附 (DVS) 和点测定进行光度评估.

主要成果:

成功合成了三种新的TMP共晶体.
与纯TMP相比,所有共晶体都表现出显著改善的高度稳定性.
TMP-DNBA共晶体表现出最高的点和卓越的稳定性,这归因于其类似网状的O-HN结结构.

结论:

晶形成是提高利古斯特拉辛 (TMP) 稳定性的有效策略.
TMP-DNBA共晶体在湿透性和热稳定性方面表现出显著的改进.
晶体结构,特别是键相互作用,在同晶体内稳定TMP方面发挥着至关重要的作用.

关键词:

青酸是什么青酸是什么协同晶体协同晶体是一个显微性是指高度的高度.利古斯特拉辛 (ligustrazine) 是一种稳定的稳定性稳定的稳定性

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