赵亚男 陈小青 朱侃 李钢. 抗癌药达沙替尼的热稳定性与晶型研究J. 药学学报, 2011,46(9): 1104-1107.
引用本文: 赵亚男 陈小青 朱侃 李钢. 抗癌药达沙替尼的热稳定性与晶型研究J. 药学学报, 2011,46(9): 1104-1107.
DIAO E-Nan, CHEN Xiao-Jing, SHU Kan, LI Gang. Thermostability and crystal structure of anticancer drug dasatinibJ. 药学学报, 2011,46(9): 1104-1107.
Citation: DIAO E-Nan, CHEN Xiao-Jing, SHU Kan, LI Gang. Thermostability and crystal structure of anticancer drug dasatinibJ. 药学学报, 2011,46(9): 1104-1107.

抗癌药达沙替尼的热稳定性与晶型研究

Thermostability and crystal structure of anticancer drug dasatinib

  • 摘要:

    本文对药物达沙替尼的热稳定性和晶型进行分析与研究。通过差示扫描量热仪 (DSC) 和热重分析仪 (TGA) 分析达沙替尼的热稳定性; 通过X射线粉末衍射仪 (XRD) 及其原位高温附件 (in situ high temperature) 测定达沙替尼试样的多晶型结构及相转变。结果表明, 达沙替尼存在两种晶型 (分子中分别含1个结晶水和1.5个结晶水), 在加热过程中两种晶型都会发生结构变化, 失去结晶水后, 最终变为相同的晶体结构, 其熔点分别为285.68 285.50

     

    Abstract:

    This article studies the thermostability and the crystal structure of a new anticancer drug dasatinib.  The thermostability of dasatinib was analyzed using the differential scanning calorimeter (DSC) and thermo gravimetric analyzer (TGA), and the structural characteristics of polymorphism and crystalline transformation was determined using the X-ray powder diffractometry (XRD) with in-situ high temperature accessories.  The results showed that dasatinib has at least two different crystal forms.  The form-I has one crystalline water and form-II one and half, and in a heating-up processing both of them would change their crystal structures.  After losing their crystalline water, both would change into the same crystalline form with no crystalline water.  Their melting points were almost the same: form- was 285.68 and form- was 285.50 .  The results of the study method would provide a comprehensive reference for the quality evaluation of dasatinib.

     

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