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两种难溶性药物-纳米多孔ZnO固体分散体的制备与提高药物溶出度机制的研究
作者姓名:Gao B  Sun CS  Zhi ZZ  Wang Y  Chang D  Wang SL  Jiang TY
作者单位:沈阳药科大学药学院;沈阳药科大学基础学院;
基金项目:国家重大基础研究发展计划(973计划)资助项目(2009CB930300)
摘    要:以自制的纳米多孔ZnO为载体制备药物固体分散体,并研究固体分散体提高药物溶出度的机制。采用熔融法分别制备吲哚美辛和西洛他唑固体分散体,扫描电镜、比表面分析仪、傅立叶红外光谱、差示扫描量热法和X-射线粉末衍射法表征结果显示纳米多孔ZnO与药物仅存在物理吸附作用,药物以无定型形式高度分散于ZnO纳米孔穴中且ZnO纳米孔穴可以抑制固体分散体中无定型药物于45℃、75%RH条件下的重结晶。体外溶出度测定结果表明,吲哚美辛固体分散体5 min时的累积溶出度可达到90%左右,西洛他唑固体分散体30 min时的累积溶出度可达到80%左右。研究探讨两种药物溶出度提高的机制与纳米多孔ZnO可增加药物分散性、控制药物以无定型形式存在并能抑制药物重结晶有关。

关 键 词:纳米多孔ZnO  吲哚美辛  西洛他唑  固体分散体  溶出度  无定型  

Preparation of two poor water soluble drugs - nanoporous ZnO solid dispersions and the mechanism of drug dissolution improvement
Gao B,Sun CS,Zhi ZZ,Wang Y,Chang D,Wang SL,Jiang TY.Preparation of two poor water soluble drugs - nanoporous ZnO solid dispersions and the mechanism of drug dissolution improvement[J].Acta Pharmaceutica Sinica,2011,46(11):1399-1407.
Authors:Gao Bei  Sun Chang-shan  Zhi Zhuang-zhi  Wang Yan  Chang Di  Wang Si-ling  Jiang Tong-ying
Institution:GAO Bei1,SUN Chang-shan1,ZHI Zhuang-zhi2,WANG Yan1,CHANG Di1,WANG Si-ling1,JIANG Tong-ying1(1.School of Pharmacy,2.School of Basic Science,Shenyang Pharmaceutical University,Shenyang 110016,China)
Abstract:Nanoporous ZnO was used as a carrier to prepare drug solid dispersion,the mechanism of which to improve the drug dissolution was also studied.Nanoporous ZnO,obtained through chemical deposition method,was used as a carrier to prepare indomethacin and cilostazol solid dispersions by melt-quenching method,separately.The results of scanning electron microscope,surface area analyzer,fourier transform infra-red spectroscopy,differential scanning calorimeter and X-ray diffraction showed that drugs were implanted ...
Keywords:nanoporous ZnO  indomethacin  cilostazol  solid dispersion  dissolution  amorphous  
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