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目的:制备奥扎格雷纳米结构脂质载体(ozagrel-loaded nanostructured lipid carriers,OZ-NLC),并考察其理化性质及体外释放。方法:采用熔融-超声乳化法制备OZ-NLC,通过正交设计法优化处方与制备工艺,使用透射电镜(TEM)、激光粒度测定仪、差示扫描量热仪(DSC)及X-射线衍射仪(XRD)考察OZ-NLC的理化性质,通过溶出试验评价其体外释放效果。结果:所制备的OZ-NLC呈球形或类球形;平均粒径为(115±10)nm;Zeta电位为(-37.6±8.9)mV;平均包封率为(61.3±5.2)%;XRD与DSC表明药物以无定形形式分散于OZ-NLC中。与奥扎格雷混悬液相比,OZ-NLC的体外溶出量明显提高且具有很好的缓释效果。结论:熔融-超声乳化法制备的OZ-NLC对促进难溶性药物奥扎格雷的口服吸收具有一定的指导价值。
OBJECTIVE: To prepare ozagrel-loaded nanostructured lipid carriers (OZ-NLC) and study its physicochemical properties and in vitro release. Methods: OZ-NLC was prepared by melt-phacoemulsification. The prescriptions and preparation techniques were optimized by orthogonal design. Transmission electron microscopy (TEM), laser particle size analyzer, differential scanning calorimeter (DSC) and X-ray diffraction The physicochemical properties of OZ-NLC were investigated by X-ray diffraction (XRD). The release of OZ-NLC was evaluated by dissolution test. Results: The prepared OZ-NLC was spherical or spheroidal with an average diameter of (115 ± 10) nm and a zeta potential of (-37.6 ± 8.9) mV. The average entrapment efficiency was (61.3 ± 5.2)%. DSC shows that the drug is dispersed in amorphous form in OZ-NLC. Compared with the oseltamivir suspension, the in vitro dissolution of OZ-NLC significantly increased and had a good sustained-release effect. CONCLUSION: OZ-NLC prepared by melt-phacoemulsification is of guiding value in promoting the oral absorption of hardly-soluble drug ozagrel.