地拉罗司-烟酰胺共晶的制备、表征及性质研究

Study on Preparation, Characterization and Properties of Deferasirox-Nicotinamide Co-crystal

摘要:
目的制备地拉罗司-烟酰胺药物共晶(物质的量之比1∶1)，提高地拉罗司溶解度。
方法以地拉罗司及烟酰胺为原料，采用研磨法，制备得到地拉罗司-烟酰胺共晶。应用¹H-NMR分析、粉末X射线衍射法、差示扫描量热法、热重法、傅里叶变换红外光谱法等对制备得到的共晶进行表征。对共晶溶解性、稳定性和引湿性进行研究。
结果相较地拉罗司原料药，共晶在水中的溶解度提高近27倍。
结论地拉罗司-烟酰胺药物共晶理化成药性良好。

Abstract:
OBJECTIVE To prepare deferasirox-nicotinamide co-crystal(molar ratio 1∶1), improve the solubility of deferasirox.
METHODS The deferasirox-nicotinamide co-crystal was prepared by the grinding method using deferasirox and nicotinamide as the raw materials. The structure of co-crystal was characterized by ¹H-NMR, power X-ray diffraction, differential scanning calorimetry, thermal gravimetric analysis and fourier transform infrared spectrum, respectively. The solubility, stability and hygroscopicity of the co-crystal were also studied.
RESULTS The solubility of co-crystal in water was increased to 27 times as compared with deferasirox.
CONCLUSION The physical and chemical properties of deferasirox-nicotinamide pharmaceutical co-crystal are good.