盐酸氟西汀胃漂浮微球的制备

The Preparation of Fluoxetine Hydrochloride Floating Microspheres

目的制备盐酸氟西汀胃漂浮微球,并对处方和制备工艺进行优化。方法采用离子凝胶法制备盐酸氟西汀海藻酸钙胃漂浮微球;以微球外观、漂浮性能以及载药量为评价指标,通过正交实验优选处方和制备工艺。结果盐酸氟西汀和海藻酸钠的比例为1∶1,玉米油量10%,羟丙基甲基纤维素0.15%,碳酸氢钠0.75%,十二烷基硫酸钠1.0%的处方载药量最大(为14.64%),微球粒径为0.9～1.1mm,起漂时间<30s,漂浮时间>8h。结论盐酸氟西汀胃漂浮微球制备工艺简便,材料易得,漂浮性能符合要求。

Objective To investigate the preparation and optimization of fluoxetine hydrochloride floating microspheres. Methods The floating microspheres composed of fluoxetine hydrochloride and calcium alginate were prepared using ion gelatin method. The appearance, buoyancy and drug loading ef- ficiency were applied to optimize the formulation and preparation procedure by orthogonal experiment. Results The results show that fluoxetine hydrochloride and sodium alginate ratio for 1 ： 1, corn oil for 10% （v/v）, hydroxypropyl methyl cellulose for 0.15 %（w/v）, NaHCOa for 0.75 % （w/v）, sodium dodecyl sulfate for 1.0% （w/v） were the best formulation which had the most drug loading efficiency （14.64%）. The average particle size of the microspheres ranged from 0.9-1.1 mm. The floating lag time was less than 30 s, and all the microspheres could float on the artificial gastric juice over 8 hours. Conclusion The technology for the preparation of fluoxetine hydrochloride floating microspheres and materials were handy. Floating properties of these microspheres can meet the requirements.