不同载体固体分散体对尼群地平和硝苯地平的增溶效果考察

Solubility Enhancement of Nitrendipine and Nifedipine with Different Carriers for Solid Dispersion

采用熔融法或溶剂法,分别以聚乙二醇(PEG)、聚维酮(PVP)、低取代-羟丙纤维素(L-HPC)、微晶纤维素(MCC)和羧甲淀粉钠(CMS-Na)为载体制备尼群地平和硝苯地平固体分散体(SD),并测定其在水及0.3%十二烷基硫酸钠(SDS)中的溶出情况。结果显示,上述载体制得的SD均可提高两种药物的溶出度。X射线衍射和扫描电镜测定结果均表明,以PVP为载体的SD中药物以无定形存在,其他载体SD中药物以微晶形式存在。扫描电镜作为固体分散体物相鉴别的手段比X射线衍射结果更直观。

The solid dispersion （SD） loaded with nitrendipine or nifedipine with polyethylene glycol （PEG）, polyvidone （PVP）, low-substituted hydroxypropyl cellulose （L-HPC）, microcrystalline cellulose （MCC） or sodium carboxymethyl starch （CMS-Na） as carrier was prepared by fusion method or solvent method, respectively. The dissolution test of above SDs was carried out in water and 0.3% sodium dodecyl sulfate （SDS） solution. The results showed that all prepared SDs could improve the drug dissolution. X-Ray diffraction （XRD） and scanning electron microscopy （SEM） were used to study the status of drug in SD. The results showed that the drug in SD with PVP as the carrier was in amorphous form, while in SD with other carriers was in microcrystalline form. The results indicate SEM was more visualized in phase identification compared with XRD.