水飞蓟宾与水杨酸、丁香酸、水杨酰胺的共晶

Cocrystals of silybin with salicylic acid,syringic acid and salicylamide

水飞蓟宾在水和脂质介质中溶解性较差,生物利用度低,而药物共晶给药技术可在不改变药物药效的前提下提高药物溶解度、溶出速率、生物利用度和稳定性等理化性质。采用溶剂蒸发法在不同溶剂中成功制备出水飞蓟宾-水杨酸、水飞蓟宾-丁香酸、水飞蓟宾-水杨酰胺3种共晶。通过X-射线衍射、傅里叶变换红外光耦等表征手段确定了共晶的形成,且对3种共晶进行溶解度测定,结果表明3种共晶增加了水飞蓟宾在水中的溶解度。

Aiming at the problems of poor solubility and low bioavailability of silybin in water and lipid medium,the pharmaceutical cocrystal technology can improve the physicochemical properties of drug solubility,dissolution rate,bioavailability and stability without changing the drug efficacy.Silybin-salicylic acid,silybin-syringic acid and silybin-salicylamide were successfully prepared by solvent evaporation in different solvents.The formation of eutectic was determined by X-ray diffraction,Fourier transform infrared optocoupler and other characterization methods,and the solubility of three kinds of eutectic was measured.The results showed that the three eutectics increased the solubility of silybin in water.