鄢雪梨 黄仁杰 肖健

    摘 要 目的：制备尼氟酸结肠靶向小球，并进行体外释药评价。方法：将尼氟酸包载于D-α-维生素E聚乙二醇1000琥珀酸酯(TPGS1000 )中形成纳米胶束，考察尼氟酸纳米胶束的包封率、载药量、粒径、Zeta电位和多分散系数(PDI)。再采用锐孔-凝固法将纳米胶束包裹于低酯果胶中形成尼氟酸结肠靶向小球，观察尼氟酸结肠靶向小球的外观形态，计算其粒径和跨距。比较尼氟酸纳米胶束和尼氟酸结肠靶向小球依次在人工胃液(2 h)、人工小腸液(3 h)和人工结肠液(3 h)中的释药情况。结果：尼氟酸纳米胶束包封率为(93.42±2.33)%、载药量为(8.54±0.36)%(n=3)，粒径为(25.8±0.6) nm、Zeta电位为(-18.73±0.23) mV(n=20)，PDI为0.25。尼氟酸结肠靶向小球外形圆整，表面纹理粗糙，其粒径为(1.33±0.14) mm(n=3)，跨距为0.26。尼氟酸纳米胶束在前5 h内的累积释放度已超过60%，而尼氟酸结肠靶向小球在前5 h内的累积释放度80%。结论：该制备方法简单可行，成功制得具有良好的结肠靶向性能的尼氟酸小球。

    关键词 尼氟酸；纳米胶束；D-α-维生素E聚乙二醇1000琥珀酸酯；结肠靶向小球；制备；体外释药

    ABSTRACT OBJECTIVE： To prepare Niflumic acid colon-targeted delivery beads， and to evaluate in vitro drug release. METHODS： Niflumic acid-loaded nanomicelles were prepared with D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS1000) as carrier material. Entrapment efficiency， drug-loading amount， particle size， Zeta potential and polydispersity coefficient (PDI) of Niflumic acid-loaded nanomicelles was investigated. The nanomicelles were encapsulated into pectin by using piercing-solidifying method to form Niflumic acid colon-targeted delivery beads. The morphology of Niflumic acid colon-targeted delivery beads was observed ......