阿司匹林鼻粘膜给药淀粉微球的制备工艺及其质量控制

Studies on preparation of aspirin-carrying starch microspheres as nasal administration and its quality evaluation in-vitro

目的 :对阿司匹林鼻粘膜给药淀粉微球的制备工艺进行考察 ,并评价其体外质量。方法 :以羧甲基淀粉钠为原料 ,对苯二甲酰氯为交联剂 ,采用界面缩聚法制备空白微球 ,用吸附载药法制备阿司匹林淀粉微球 ,并对其形态、载药量、包封率、体外释放度等进行了研究。结果 :微球形态圆整 ,大小均匀 ,粒径在 2 0～ 10 0 μm ,平均粒径为5 3.5 4μm,载药量 16 .6 5 % ,包封率92 .5 % ,体外释药符合Weibull方程。结论 :本微球制备工艺较简便 ,各种因素较易控制 ,重现性好 ,载药量与包封率均较高 。

OBJECTIVE To study the preparation of aspirin-carrying starch microspheres as nasal administration and evaluate its quality in-vitro. METHODS The microspheres were prepared through interfacial cross-linking of CMS-Na. The morphology,drug-loading rate,embedding rate and dissolution in-vitro were observed. RESULTS The microspheres were spherical with average size of 53.54 μm. Loading capacity was found to be 16.65% while entrapment rate was 92.5%. Its release character in-vitro could be described by Weibull equation.CONCLUSIONS The microspheres were shown to entrap aspirin with a high efficiency and apply to nasal administration.