目的 制备磺胺嘧啶固体分散体,考察其溶解度和体外溶出度,并对物相进行鉴定。方法 以体外溶出度为指标,利用单因素试验与正交设计试验优化固体分散体的制备工艺。采用差示扫描量热法(DSC)、红外光谱法和粉末X-射线衍射法鉴定药物在固体分散体中的存在状态。结果 以最佳工艺制备的磺胺嘧啶固体分散体,与原料药相比药物溶解度提高了17倍,溶出速率提高了3倍;物相鉴定表明,药物在分散体中主要以无定型状态存在。结论 以PEG4000为载体,采用溶剂熔融法制备的磺胺嘧啶固体分散体,可显著提高磺胺嘧啶的溶解度和溶出速率。
Abstract
OBJECTIVE To prepare sulfadiazine solid dispersion, determine its solubility and dissolution in vitro, and investigate its physical properties. METHODS Using in vitro dissolution as an index, single factor test and orthogonal design were used to optimize the preparation process of sulfadiazine solid dispersion. The existing state of sulfadiazine was identified by DSC, IR spectroscopy, and powder X-ray diffraction. RESULTS The solubility and dissolution rate of sulfadiazine solid dispersion prepared by the optimized preparing process were increased by 17 times and 3 times respectively than crude sulfadiazine. Sulfadiazine existed in an amorphous state as shown by phase identification. CONCLUSION The solid dispersion prepared by the solvent-molten method with PEG4000 as the carrier can significantly improve the solubility and the dissolution rate of sulfadiazine.
关键词
磺胺嘧啶 /
固体分散体 /
溶出度 /
正交设计 /
表征
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Key words
sulfadiazine /
solid dispersion /
dissolution rate /
orthogonal design /
characterization
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中图分类号:
R944
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参考文献
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脚注
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基金
国家级星火计划资助项目( 2015GA780040)
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