艾拉莫德两种晶型的体内外比较研究
Comparative study on the two crystal forms of iguratimod
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摘要: 对艾拉莫德两种晶型(α晶型和β晶型)进行体内外比较研究。分别制备不同晶型的艾拉莫德，利用差式扫描量热仪、X线粉末衍射仪(XRPD)等分别考察α和β两种晶型的熔点、微观形态、密度、溶解度和稳定性等理化性质，通过对大鼠灌胃给予不同晶型艾拉莫德，考察其体内吸收情况。实验表明:α晶型与β晶型具有相似的熔点及溶解性质；大鼠体内生物学表现基本相同；但β晶型比α晶型具有更好的流动性及可压性，因此，β晶型更适用于固体制剂的开发。Abstract: The aim of this study was to compare the physicochemical properties and in vivo behavior of two crystal forms of iguratimod. The different crystal forms of iguratimod were prepared and their physicochemical properties were studied by DSC and XRPD. The absorptions of the crystal forms α and β was compared by administering iguratimod to SD rats. It was found that the melting points and solubilities, as well as pharmacokinetic parameters of crystal forms α and β were similar. No significant difference was found in biological activity in the rats between them. Meanwhile, the flowability and compressibility of crystal form β were better than those for form α. Therefore, the crystal form β is more suitable for the development of solid formulation.
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Keywords:
- iguratimod /
- polymorphs /
- physicochemical property /
- pharmacokinetics
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