沙美特罗白蛋白微球的制备与体外释放度考察

目的:制备沙美特罗白蛋白微球,并考察其体外释放性能。方法:以白蛋白为载体,采用乳化交联法制备沙美特罗白蛋白微球。在单因素考察的基础上,利用正交设计优化沙美特罗白蛋白微球制备工艺,并对微球的粒径,形态,体外释放特性进行研究。结果:制得的微球形态圆整,平均粒径为（16.82±1.25）μm,平均载药量为（52.08±3.26）%,平均包封率为（60.54±3.17）%,体外释放符合Higuchi方程,Q=11.5846t_1/2-1.207（r=0.9985）。结论:沙美特罗白蛋白微球体外释放特性符合长效制剂特征。

Preparation and in vitro Release of Salmeterol Albumin Microspheres

Objective： To prepare salmeterot albumin microspheres and evaluate the release behavior in vitro. Method ： The micro- spheres were prepared by emulsion chemical cross-linking method using albumin as the wall material. Based on the result of single factor experiment, the preparation methods were evaluated by orthogonal experiment. The mean diameter and size distribution, drug loading, en- trapment efficiency and in vitro release property of the optimized microspheres were examined. Result： The microspheres were spherical and the surface was smooth. The average particle size was （ 16. 82 ± 1.25 ） μm, drug loading rate was （ 52. 08 ± 3.26） % and entrap- ment efficiency was （60. 54 ±3.17） %. The drug release in vitro could be described by Higuchi equation ： Q = 11. 584 6 t1/2 - 1. 207 （ r = 0. 998 5）. Conclusion： The salmeterol albumin microspheres show the sustained release property in vitro.