目的 尝试采用一种新型技术制备人参皂苷Rg3固体分散体,从而提高脂、水难溶药物人参皂苷Rg3的溶解性。方法 以醋酸羟丙基甲基纤维素琥珀酸酯为载体制备人参皂苷Rg3固体分散体,利用傅立叶变换近红外光谱、X-射线衍射、差示量热扫描分析及扫描电子显微镜等分析方法表征人参皂苷Rg3固体分散体。利用高效液相色谱法分别测定了人参皂苷Rg3和人参皂苷Rg3固体分散体的平衡溶解度。结果 人参皂苷Rg3固体分散体可以增加药物的溶解度,在模拟人十二指肠和空肠pH的条件下人参皂苷Rg3固体分散体的溶解性能显著优于原料药。结论 本实验制备人参皂苷Rg3固体分散体的方法操作简单、经济实用,增加人参皂苷Rg3溶解度的效果显著。
Abstract
OBJECTIVE To prepare ginsenoside Rg3 (G-Rg3) solid dispersion by atoping a new technology to increase the solubility of G-Rg3. METHODS Hydroxypropyl methylcellulose acetate succinate (HPMCAS) was selected as the carrier to prepare G-Rg3 solid dispersion. The G-Rg3 solid dispersion was characterized via Fourier transform infrared spectroscopy, X-ray diffractometry, differential scanning calorimetry analysis, and scanning electron microscopy. The equilibrium solubility of G-Rg3 and G-Rg3 solid dispersion were measured by using high-performance liquid chromatography. RESULTS The G-Rg3 solid dispersion was successfully prepared. The solubility of G-Rg3 solid dispersion in the weak acid medium (pH 5.5 and 6.4) designed to simulate human duodenum and jejunum was significantly higher than that of G-Rg3. CONCLUSION The preparation method of G-Rg3 solid dispersion is simple, economic, and practical, which can obviously increase the of solubility of G-Rg3.
关键词
人参皂苷Rg3 /
固体分散体 /
醋酸羟丙基甲基纤维素琥珀酸酯 /
溶解度
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Key words
ginsenoside Rg3 /
solid dispersion /
hydroxypropyl methylcellulose acetate succinate /
solubility
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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
国家自然科学基金资助项目(81102394);中国博士后科学基金(2013M530899)
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