姜黄素赖氨酸共晶的制备及不同晶型溶解性对比

Preparation of Curcumin-Lysine Cocrystal and Solubility Comparison of Different Crystal Forms

目的:开发一种姜黄素药物共晶,以改善姜黄素生物利用度低、成药性差的问题。方法:采用溶剂结晶法,制备姜黄素-赖氨酸共晶,并培养得到a、b两种晶型。通过元素分析、差示扫描量热分析、X射线衍射法分别对其进行表征。测定上述两种晶型的溶解曲线,同姜黄素作对比。结果:姜黄素与赖氨酸按照1∶1的化学计量比结合,形成共晶,得到的共晶溶解性能明显优于姜黄素。结论:姜黄素-赖氨酸共晶具有良好的成药性可作为新的化学实体进行后续开发。

Objective ： To develop a new cocrystal form to improve bioavailability and druggability of curcumin. Methods： Solvent crystallization was used to prepare curcumin-lysine cocrystal, and two crystal forms （ a and b） were obtained. The two cocrystal forms were characterized by elemental analysis, differential scanning calorimetry and X-ray diffraction. The dissolution profiles of the two crystal forms were detected and compared with that of curcumin. Results： Curcumin combined with lysine at a stoichiometry of 1 ： 1 to form the cocrystal with much better solubility than curcumin. Conclusion： Curcumin-lysine cocrystal has ideal druggability, which means the cocrystal can be a new chemical entity used for subsequent development.