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。
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 into nanopores of ZnO by physical adsorption effect and highly dispersed into nanopores of ZnO in amorphous form,moreover,these nanopores strongly inhibited amorphous recrystallization in the condition of 45 ℃ and 75% RH.In addition,the results of the dissolution tested in vitro exhibited that the accumulated dissolutions of indomethacin and cilostazol solid dispersions achieved about 90% within 5 min and approximately 80% within 30 min.It was indicated in this study that the mechanism of drug dissolution improvement was associated with the effects of nanoporous ZnO carrier on increasing drug dispersion,controlling drug in nanopores as amorphous form and inhibiting amorphous recrystallization.
出处
《药学学报》
CAS
CSCD
北大核心
2011年第11期1399-1407,共9页
Acta Pharmaceutica Sinica
基金
国家重大基础研究发展计划(973计划)资助项目(2009CB930300)
