京尼平-β-环糊精包合物制备工艺研究

Study on Preparation Process of Inclusion Complex of Genipin-β-Cyclodextrin

目的研究京尼平-β-环糊精包合物最佳制备工艺。方法采用研磨法,以包合物的含量和京尼平(genipin,GP)收率为考察指标,通过正交实验设计,综合平衡后确定最佳制备工艺。结果最佳包合条件为:包合时间1 h、GP和β-环糊精的配比(摩尔比)1∶1、包合溶剂为水。经红外光谱法、紫外光谱法、电镜扫描法、X-射线衍射法和相溶解度法鉴定,确证形成京尼平-β-环糊精包合物。结论采用最优包合条件制备的包合物收率为76.27%,京尼平含量为16.5 mg·g-1。制成包合物后提高了京尼平的稳定性,制备工艺简单,同时也为京尼平制备成各种剂型开辟良好的前景。

OBJECTIVE To select the optimum preparation process of inclusion complex of genipin-β-cyclodextrin. METHODS The inclusion compound was prepared by the trituration method. The multiple factor and levels experiments were done by orthogonal design with the recovery of inclusion complex and the content of genipin as criteria. RESULTS The optimum entrapment conditions were as follows： the reaction time was 1 h, the molar ratio of genipin to β-cyelodextrin was 1 ： 1, the solution was water. The formation of compound genipin-β-cyelodextrin was confirmed by infrared spectroscopy, ultraviolet spectra, scanning electron microscopy （ SEM）, X-ray diffractometry and Phase Solubility Method. CONCLUSION The recovery of inclusion complexm prepared with the optimum inclusion condition was 76. 23% and the content of genipin was 16. 5 mg·g^-1. The stability of genipin was enhanced. Meanwhile, such inclusion complex may be fuller developed into a lot of preparations.