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用改良的冷冻融溶法制备出碘醚柳胺(Rafoxanide,Raf)脂质体定向剂,并对其药物特性进行了观察与测定。用Raf与聚乙烯吡咯烷酮(Polyvinylpyrolidone,PVP)共沉法解决了Raf在水性介质中不溶的问题,从而为制备该药脂质体创造了必要条件。采用单因素比较法优选出制备碘醚柳胺脂质体的最佳处方组成:药脂比为1∶27(w/w);Pc与Chol比为2∶1(mol/mol)。结果显示,用此法制备的脂质体包封率可高达58%;电镜下显示以多层脂质体为主,粒径大者4μm~6μm,小者0.1μm~1.0μm,后者约占60%。在室温条件下贮存75d后,其包封率由原来的56.97%下降到51.83%,表明用本法制备的脂质体具有良好稳定性。
Rafoxanide (Raf) liposome targeting agent was prepared by a modified freeze-thaw method, and its drug properties were observed and determined. The Raff and polyvinylpyrrolidone (PVP) co-precipitation method to solve the problem of insoluble in aqueous media Raf, thus preparing the drug liposomes created the necessary conditions. The optimum formulation of lipiodol ether liposomes was optimized by single factor comparison method. The ratio of drug to lipid was 1:27 (w / w); the ratio of Pc to Chol was 2:1 (mol / mol). The results showed that the encapsulation efficiency of liposomes prepared by this method was as high as 58%. The results of electron microscope showed that the liposomes were mainly composed of multilamellar liposomes with the size of 4μm ~ 6μm and the smaller ones of 0.1μm ~ 1.0μm. About 60%. After 75 days of storage at room temperature, the entrapment efficiency decreased from 56.97% to 51.83%, indicating that liposomes prepared by this method have good stability.