目的由于单一载体材料包封药物,易于形成高度结晶的颗粒将药物排出晶格,使传统SLN载药量和包封率较低,为此本实验室运用固、液态复合载体材料制备了包载药物雷公藤内酯醇的新型SLN。方法运用4种包封率测定方法对雷公藤内酯醇在7种载体材料中的包封性能进行考察,结合微观分析手段TEM(透射电子显微镜)和AFM(原子力显微镜)以及激光粒度(LD)和Zeta电位对新型SLN物化性能进行表征。结果发现以液体状态存在的三辛酸甘油酯对药物的包封能力较好,拥有混合载体材料结构Compritol ATO 888对雷公藤内酯醇的包封率亦较高,而运用上述2种复合载体材料制备的雷公藤内酯醇新型SLN更获得高达93%的包封率。TEM和AFM形貌观察,颗粒呈球状,比较规则,平均粒径102 nm,Zeta电位低于-25mV,冰箱长期留样研究表明系统比较稳定。结论最终选择Compritol ATO 888和三辛酸甘油酯作为复合载体材料制备雷公藤内酯醇新型SLN载体系统。
The orthogonal design was used to optimize the formulation of helicid orally disintegrating tabletsprepared by direct powder compression method. The optimized formulation was as follows: weight ratio ofpolyvinylpolypyrrolidone and low-substituted hydroxypropylcellulose 1∶1; the amount of NaHCO3-citric acid(1∶1)14% and microcrystalline cellulose 10%. The prepared tablets disintegrated completely within 30s, dissolved in 2min andtasted fine.
