霉酚酸酯羟丙基-β-环糊精包合物的制备

Preparation of Mycophenolate Mofetil Hydroxypropyl-β-cyclodextrin Inclusion Complexes

目的:优化霉酚酸酯羟丙基-β-环糊精(HP-β-CD)包合物的包合工艺。方法:选用溶液-搅拌法制备包合物,采用正交试验来筛选影响HP-β-CD包合的主要因素,即HP-β-CD与药物的比例、包合温度、包合时间和搅拌速度,并以包封率和回收率为考察指标进行优选制备工艺,通过DSC验证包合物。结果:霉酚酸酯HP-β-CD的最佳包合条件为:HP-β-CD与药物配比为1:1,包合温度为80℃,包合时间为3h,搅拌速度为400 r.min^(-1)时,霉酚酸酯HP-β-CD包合物的包合工艺最佳。结论:霉酚酸酯羟丙基-β-环糊精(HP-β-CD)包合物的制备方法简便、可靠,并可大大提高霉酚酸酯的溶解度。

Objective： To optimize preparation process of mycophenolate mofetil hydroxypropyl -β- cyclodextrin （ HP-β-CD） inclusion complexes. Method： Inclusion complexes were prepared by solution-stirring methods. The optimum clathration condition was selected by orthogonal test with the ratio of HP-β-CD to mycophenolate mofetil, the clathration times and stirring speed as factors. And the encapsulation and clathration recovery were used as indexes. Result： The optimum preparation condition was as follows ： the ratio of HP-β-CD to mycophenolate mofetil was 1： 1, the inclusion temperature was 80℃ , the inclusion time was 3h, and the stirring speed was 400 r. min ^- 1. Conclusion ： The method of preparation of mycophenolate mofetil hydroxypropyl -β- eyclodextrin inclusion complex is convenient and reliable, and it can apparently improve the solubility of myeophenolate mofetil.