注射用伊潘立酮长效缓释微球的制备和评价

Preparation and evaluation of iloperidone loaded PLGA microspheres

目的制备伊潘立酮的PLGA微球,并进行质量评价。方法建立HPLC方法测定伊潘立酮的含量;比较5种规格的PLGA作为载体材料对微球质量的影响;运用正交实验设计优化处方组成和制备工艺。结果 PLGA的种类对伊潘立酮微球的包封率和体外释放有显著影响。按照正交设计得到优化处方制备的微球,形状圆整,平均粒径为(27.3±2.7)μm,包封率为84.4%,体外释放试验第1天累计释放17.6%,28 d的累计释放度为85.7%,释药曲线符合Higuchi释放模型。结论本实验制备得到的伊潘立酮微球的包封率较高,没有明显的突释,具有较好的缓释效果。

Objective To prepare iloperidone loaded PLGA microspheres and evaluate its pharmaceutical characters. Methods The HPLC method was established to determine the concentration of iloperidone. The effect of 5 kinds of specifications of PLGA as carrier material on the quality of the microspheres was investigated. The formulation and the preparation conditions were optimized by orthogonal tests. Results The kinds of PLGA and drug encapsulation efficiency showed Significant effect on the property of the microspheres, in particular on the release rate. The best formulation was obtained according to the effects of different factors on the preparation of iloperidone microspheres. The formed microspheres were spherical with smooth surface and the average size was （27.3±2.7） μm. The drug encapsulation efficiency was 84.4%. In vitro release study revealed of 17.6% at the first day and 85.7% of drug released from PLGA microspheres in 28 d. The release kinetics of microspheres in vitro were characterized by Higuchi equation. Conclusion Iloperidone-eontaining PLGA microspheres are prepared successfully with high encapsulation efficiency, with no obvious sudden release and good sustained release characteristics.