关键词：
金雀异黄酮;固体分散体;纳米;聚乙烯吡咯烷酮;累积溶出率
摘 要：
为提高金雀异黄酮(genistein,GEN)的溶解度,选用聚乙烯吡咯烷酮(polyvinylpyrrolidone,PVP)K30为载体,采用旋转蒸发法制备金雀异黄酮纳米固体分散体(GEN-PVP K30 SD);通过粉末X射线衍射、差示扫描量热和体外溶出试验筛选最佳比例;利用傅里叶变换红外光谱、扫描电子显微镜和动态光散射对固体分散体进行表征,并进行稳定性研究.结果显示,在粉末X射线衍射和差示扫描量热分析中,不同药载比(1∶3、1∶5、1∶7、1∶9)的旋蒸样品均无GEN晶体特征峰和吸热峰,表明GEN以无定形态分散于载体,固体分散体制备成功;GEN的累积溶出率仅为0.17%,不同药载比固体分散体的累积溶出率分别为20%、46%、82%、99%;药载比1∶9的样品黏度大,因此最佳选择为药载比1∶7.红外结果显示,GEN与载体间产生了氢键;GEN-PVP K30 SD为不规则的块状结构,粒径为156 nm±3 nm,且GEN-PVP K30 SD在180 d内稳定性良好.结果表明,通过旋转蒸发法成功制备了金雀异黄酮纳米固体分散体,累积溶出率显著高于GEN.
译 名：
Studies on Preparation and Properties of Genistein Nano-solid Dispersion
关键词：
genistein%solid dispersion%nano%polyvinylpyrrolidone%cumulative dissolution
摘 要：
To improve the solubility of genistein(GEN),polyvinylpyrrolidone K30(PVP K30)was chosen as the carrier in this study,and the genistein nano-solid dispersion(GEN-PVP K30 SD)was prepared by solvent rotary evaporation.The optimal ratio of GEN and carrier was screened through powder X-ray diffraction,differential scanning calorimetry and dissolution test.The prepared solid dispersions were also characterized using fourier transform infrared spectrometer,scanning electron microscopy,dynamic light scatteringand stability studies.The results showed that there were no characteristic peaks of GEN in the rotary evaporation samplesin powder X-ray diffraction and differential scanning calorimetry analysis,indi-cating that GEN was dispersed in the carrier as an amorphous form and the solid dispersions were prepared successfully.The cumulative dissolution rate of GEN was only 0.17%,and the cumulative dissolution rate of solid dispersions with different drug loading ratios(1∶3,1∶5,1∶7,1∶9)were 20%,46%,82%,and 99%,respevtively.The viscosity of solid dispersion with a drug loading ratio of 1∶9 is high,therefore,the best choice is a drug loading ratio of 1:7.Infrared results showed hydrogen bonding formed between GEN and PVP K30.GEN-PVP K30 SD was irregularly blocky and the particle size was 156±3 nm.GEN-PVP K30 SD remained amorphous for 180 d.The results showed that the genistein nano-solid dispersion was successfully prepared by solvent rotary evaporation method.The cumulative dissolution rate was significantly higher than that of GEN.
