RESUMO
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.
RESUMO
Objective:To optimize the extraction process of Ilex chinensis Sims by Box-Behnken response surface method. Meth-ods:The HPLC determination of pedunculoside was performed and validated. With the extraction rate of pedunculoside as the index, the influencing factors including material-liquid ratio, ethanol concentration, reflowing temperature and decocting frequency were opti-mized by Box-Behnken response surface method. Results:The optimized parameters were as follows:the material/liquid ratio was 1:10, the ethanol concentration was 70%, the ultrasonic temperature was 80℃,and the decocting frequency was three times. Conclu-sion:The HPLC method and the best extraction conditions are reliable.
RESUMO
Recently,the screening technologies of pharmaceutical cocrystals have become a research focus of improving drug solubility and stability. The technique changes medicine properties by intermolecular forces without changing the molecular structure , which provides new ways for the development of the insoluble drug. In addition,the formation of cocrystal gives new properties to drugs and intellectual property rights are effectively protected. This review focuses on screening technique ,which provides references for fur?ther studies of pharmaceutical cocrystal.