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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-cyclodextrin (MSZ-HP-β-CD) inclusion complex and investigate its properties. Methods: MSZHP-β-CD inclusion compound was prepared by stirring method, and the content of MSZ was determined by HPLC. Orthogonal test method was used to optimize the preparation process of MSZ-HP-β-CD inclusion complex with inclusion rate and inclusion compound yield as the comprehensive index. The inclusion complex was verified by UV, X-ray diffraction and solubility method, and its dissolution was investigated. Results: The MSZ-HP-β-CD inclusion complex was prepared by stirring at a temperature of 35 ℃ with a mass ratio of MSZ to HP-β-CD of 1: 4 (mg / g) The average inclusion rate was 96.28%, the average inclusion rate was 97.87%, and the freeze-dried powder was identified as inclusion complex. Compared with MSZ, the dissolution of MSZ inclusion significantly increased, and the cumulative dissolution reached 98% at 10 min. CONCLUSION: The MSZ-HP-β-CD inclusion complex prepared under optimal conditions has good reproducibility and process stability, and can significantly improve the dissolution rate of MSZ.