【摘要】 目的延缓洛索洛芬钠在局部的作用时间,了解洛索洛芬钠缓释微球的体外释药特性。方法采用乳化-化学交联法制备明胶微球,采用正交试验优化明胶微球的处方和制备工艺;采用流化床包衣技术制备缓释微球;采用透析法考察体外释药特性。结果制备明胶微球最优处方和工艺为:洛索洛芬钠5.0 g,质量分数为20%的明胶溶液100 mL作为水相,含质量分数0.5%Span 80的液体石蜡混合液400 mL作为油相,55℃搅拌下将水相缓缓加入至油相中,500 r.min-1乳化20 min,冰水浴20 min,加入戊二醛使体积分数为50%,交联90 min,4000 r.min-1离心分离10 min,用丙酮、乙醚交替洗涤3次,40℃真空干燥12 h;制备的明胶微球平均粒径为18.25μm,载药量为19.37%,包封率为87.72%,包衣后质量增加25%;洛索洛芬钠缓释微球体外释药过程符合Higuchi方程。结论制备的洛索洛芬钠缓释微球具有明显的缓释作用。更多还原

【Abstract】 Objective To prepare sustained-release microspheres of loxoprofen sodium,and investigate its in vitro release property.Methods The microspheres were prepared by emulsify-chemical cross linking method,and its formulation and technique were optimized by means of orthogonal experiments.Fluid-bed coating technique was utilized to prepare sustained-release microspheres.The dialysis method was used to investigate its in vitro release property.Results The optimum formulation and technique to prepare the gelatin microspheres were determined as follows:Loxoprofen sodium(5.0 g)was added to the 20%(m ∶m)gelatin solution(100 mL)as the water phase,paraffin oil(400 mL)within 0.5%(m∶m)Span 80 was made to be the oil phase,then the water phase was added slowly to the oil phase at 55 ℃ under constant stirring using a mechanical stirrer at the rotation speed of 500 r·min-1 for emulsifying of 20 min.Glutaral was added to the emulsion made its concentration of 50%(V ∶V)to crosslink for 90 min in order to form solid microspheres after iced bath of 20 min.The microspheres was centrifuged at 4 000 r·min-1 to isolate the solid microspheres,and then washed alternately using acetone and ether for three times,and dried by vacuum drying oven for 12 h to obtain dry microspheres.The microspheres prepared by the selected procedure had a mean diameter of 18.25 μm.The drug loading was about 19.37%,and the entrapment efficiency was 87.32%.The weight of coating of sustained-release microspheres was increased by 25%,and its in vitro release profile property fitted the Higuchi equation.Conclusion The sustained-release mirospheres prepared by the selected procedure have distinct sustained release action.更多还原