多孔淀粉泡沫改善达比加群酯的溶出速率

徐杰,赵文明,吴超,赵宗哲,郝艳娜,赵颖

中国药学杂志 ›› 2015, Vol. 50 ›› Issue (16) : 1408-1411.

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中国药学杂志 ›› 2015, Vol. 50 ›› Issue (16) : 1408-1411. DOI: 10.11669/cpj.2015.16.010
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多孔淀粉泡沫改善达比加群酯的溶出速率

  • 徐杰,赵文明*,吴超*,赵宗哲,郝艳娜,赵颖
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Preparation of Porous Starch Foam to Improve the Dissolution Rate of Dabigatran Etexilate

  • XU Jie, ZHAO Wen-ming*, WU Chao*, ZHAO Zong-zhe, HAO Yan-na, ZHAO Ying
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摘要

目的 制备多孔淀粉泡沫改善达比加群酯的溶解度和溶出速率。方法 通过溶剂交换法制备多孔淀粉泡沫(PSF),并以多孔淀粉泡沫为载体,通过溶剂挥发法将达比加群酯(DE)载入多孔淀粉泡沫纳米孔道中。使用扫描电镜观察载体多孔淀粉泡沫的形态和结构,应用差示扫描量热法,X射线衍射法和傅里叶红外光谱法鉴别载药样品(PSF-DE)中达比加群酯的分散状态,并通过体外溶出实验考察其体外溶出度。结果 结构表征证明成功制备了多孔淀粉泡沫,并且多孔淀粉泡沫纳米孔道的空间抑制效应有效抑制了达比加群酯的结晶。体外溶出实验表明,达比加群酯的溶出速率得到显著提高。结论 多孔淀粉泡沫改善了水难溶性药物达比加群酯的亲水性。

Abstract

OBJECTIVE To prepare porous starch foam to improve the solubility and dissolution rate of dabigatran etexilate. METHODS Porous starch foam(PSF)was synthesized as a carrier by solvent exchange method. Dabigatran etexilate (DE) was loaded onto the nanopores of PSF by solvent evaporation method. Scanning electron microscopy was used for investigating the morphology and structure of PSF. The dispersal state of DE in drug-loaded sample (PSF-DE) was determined by differential scanning calorimetry, powder X-ray diffraction and fourier transform infrared spectroscopy. The dissolution rate was measured by in-vitro dissolution experiment. RESULTS Porous starch foam was prepared successfully and the spatial restriction of nanopores effectively suppressed crystallinity of dabigatran etexilate as shown by structure characterization. The in-vitro dissolution experiment showed that the dissolution rate of dabigatran etexilate was improved significantly. CONCLUSION Porous starch foam can improve the hydrophilicity of the poorly water-soluble drug dabigatran etexilate.

关键词

多孔淀粉泡沫 / 生物降解材料 / 达比加群酯 / 水难溶性药物 / 溶出速率

Key words

porous starch foam / biodegradable material / dabigatran etexilate / poorly water-soluble drug / dissolution rate

引用本文

导出引用
徐杰,赵文明,吴超,赵宗哲,郝艳娜,赵颖. 多孔淀粉泡沫改善达比加群酯的溶出速率[J]. 中国药学杂志, 2015, 50(16): 1408-1411 https://doi.org/10.11669/cpj.2015.16.010
XU Jie, ZHAO Wen-ming, WU Chao, ZHAO Zong-zhe, HAO Yan-na, ZHAO Ying. Preparation of Porous Starch Foam to Improve the Dissolution Rate of Dabigatran Etexilate[J]. Chinese Pharmaceutical Journal, 2015, 50(16): 1408-1411 https://doi.org/10.11669/cpj.2015.16.010
中图分类号: R944   

参考文献

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基金

辽宁省大学生创新创业训练计划资助项目(201310160027);校长基金-奥鸿博泽基金-医药创新专项资助项目(XZJJ20130104-07)
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