摘要
目的 探讨氯化血红素 β环糊精包合物的制备工艺及包合前后氯化血红素物理性质的变化情况。 方法 采用研磨法制备氯化血红素 β环糊精包合物 ,运用正交试验法优选最佳制备工艺 ,并用差示热分析图谱、红外光谱、紫外光谱的变化验证包合物的形成 ;测定其溶解度和溶出度。结果 试验结果表明 ,最佳制备工艺条件为氯化血红素 :β 环糊精 (摩尔比 ) 1∶8、研磨时间 80min ,氯化血红素 :稀氨水 (g :mL) 1∶10 ,β环糊精 :水 (g :mL) 1∶30 ;氯化血红素经 β环糊精包合后 ,溶解度为原药的 7.2 8倍 ,氯化血红素及包合物的溶出度参数t50 分别为 6 7.0 ,19.7min ,经红外光谱、紫外光谱、差示热分析法确证了包合物的形成。结论 包合后氯化血红素的溶解度和溶出度均有显著提高 ,并掩盖了其不良气味 ,证实氯化血红素和 β环糊精形成了新的物相 ,提示本工艺可行 。
OBJECTIVE: To study the preparation process of the inclusion complex of hemin-β-cyclodextrin and the changes of the physical properties of hemin before and after being included by β-cyclodextrin. METHOD: The inclusion complex of hemin-β-cyclodextrin was prepared by milling method. The best preparation process of hemin-β-cyclodextrin was optimized with orthogonal experiments. The solubility and dissolution of inclusion complex and hemin were measured. RESULTS: The optimum preparation process of hemin-β-cyclodextrin was as following: the ratio of hemin to β-cyclodextrin was 1:8, the ratio of hemin to dilute ammonia solution was 1:10, the ratio of β-cyclodextrin to water was 1:30 and milling for 80 min. The solubility of hemin in the inclusion complex was 7.28 times higher than that of pure hemin. The parameters of dissolution of hemin and inclusion complex t50 were 67.0 min and 19.7 min, respectively. CONCLUSION: A new physical phase was formed between hemin and β-cyclodextrin. The solubility and dissolution of hemin was increased, and the bad smell of hemin was overcome after being included by β-cyclodextrin. Meanwhile, such inclusion complex may be further developed into a lot of preparations.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2001年第6期389-391,共3页
Chinese Pharmaceutical Journal
