伊曲康唑共晶的制备与表征

Preparation and characterization of itraconazole cocrystals

目的制备与表征难溶性药物伊曲康唑共晶,并考察其对药物溶解度和溶出度的影响。方法采用溶剂研磨法制备了伊曲康唑与丙二酸、丁二酸、苹果酸和酒石酸的四种共晶,应用差示扫描量热分析(DSC)、热重分析(TGA)、X射线衍射(XRD)和红外光谱(IR)对其进行表征。结果伊曲康唑和上述4种共晶形成物之间形成了共晶,与伊曲康唑原料药相比,形成的共晶具有较高的溶解度和溶出度。结论共晶技术在提高难溶性药物溶解度和溶出度方面具有广阔的应用前景。

Objective To prepare and characterize itraconazole cocrystals and investigate its effect on solubili- ty and dissolution properties. Methods Itraconazole cocrystals with malonic acid, succinic acid, malic acid and tartaric acid were prepared by liquid-assisted （solvent-drop） co-grinding method, respectively. The co- crystals were characterized by differential scanning calorimetric（ DSC）, thermogravimetric analysis （TGA）, X-ray diffraction（XRD） and infrared absorption spectroscopy （1R）. Results The results indicated the cocrys- tal formation of itraconazole with four different coformers. Moreover, the cocrystals displayed higher appar- ent solubilities and better dissolution than itraconazole powders. Conclusions The cocrystal technology has been demonstrated potential in improving the solubility and dissolution of water insoluble drugs.