美沙拉嗪羟丙基-β-环糊精包合物的制备及其性质研究  

Preparation and Properties of Mesalazine Hydroxypropyl-β-cyclodextrin Inclusion Complexes

作　　者：李卫华[1] 宋兴龙 

机构地区：[1]枝江市人民医院药剂科,湖北枝江443200 [2]湖北保康县人民医院药剂科

出　　处：《中国药师》2016年第9期1679-1682,共4页China Pharmacist

摘　　要：目的:制备美沙拉嗪羟丙基-β-环糊精(MSZ-HP-β-CD)包合物,并对其进行性质考察。方法:采用搅拌法制备MSZHP-β-CD包合物,以HPLC法测定MSZ的含量。采用正交试验法,以包合率和包合物收率为综合指标,优化MSZ-HP-β-CD包合物的制备工艺。采用紫外、X射线衍射及溶解度法对包合物进行验证,并对其溶出度进行考察。结果:采用搅拌法,在温度35℃、MSZ与HP-β-CD质量比为1∶4(mg/g)、包合时间3 h的条件下制备MSZ-HP-β-CD包合物。经验证平均包合率达96.28%,平均包合物得率达97.87%,其冻干粉经鉴别已形成包合物。与MSZ相比,MSZ包合物的溶出度显著提高,10 min时累积溶出度达到98%以上。结论:以最佳工艺条件制备的MSZ-HP-β-CD包合物重复性好,工艺稳定,能显著提高MSZ的溶出度。Objective： To prepare mesalazine hydroxypropyl-β-cyelodextrin （MSZ-HP-β-CD） inclusion complexes and observe the properties. Methods： The inclusion complexes were prepared by a stirring method and the content of MSZ was determined by HPLC. The preparation technology was optimized by orthogonal test with the inclusion rate and the yield of inclusion complexes as the indices. The inclusion complexes were identified respectively by ultraviolet （UV） spectrometry, X-ray diffraction （XRD） and solubility. The dissolution rate was investigated. Results： Using the stirring method, the optimum preparation process was as follows： the inclusion temperature was 35 ℃, the ratio of MSZ to HP-β-CD was 1 ： 4 （ mg/g）, and the inclusion time was 3 h. The average inclusion rate of the complexes was 96.28%, and the yield was 97.87%. The identification results showed that the freeze-dried powder was inclusion complexes. Compared with that of MSZ, the dissolution of MSZ- HP-β-CD inclusion complexes was notably enhanced. Conclusion： The prepared MSZ-HP-β-CD with optimized technology has good reproducibility and stable technology, which can obviously improve the dissolution of MSZ.

关 键 词：美沙拉嗪 羟丙基-Β-环糊精 包合物 制备 性质 

分 类 号：R944.9[医药卫生—药剂学]