挤出滚圆法制备马来酸曲美布汀胃黏附微球

目的利用适合于工业化生产的方法制备具有较好生物黏附能力和适宜缓释效果的马来酸曲美布汀胃黏附微球。方法通过挤出滚圆法制备马来酸曲美布汀胃黏附微球 ;以动物体内外胃黏膜表面滞留程度 ,考察CP的含量和微球粒径对微球黏附能力的影响 ;以体外释药速率评价热处理 ,CP的含量 ,CP、SA与EC间的比例 ,TM含量 ,微球粒径对微球缓释效果的影响 ;以镇痛效果考察最终处方的药效。结果CP比例增加 ,微球的黏附性增强 ,药物缓释效果降低 ,呈现负相关 ;TM含量增加 ,微球的黏附性降低 ,缓释效果降低 ;微球粒径增大 ,微球的黏附性降低 ,缓释效果增加 ;最佳处方的作用时间延长 ,作用强度增强。结论载药量在 2 0 % (w)以下 ,粒径为 5 0 0～ 90 0 μm,CP含量为 1 3 3 0 % (w)的TM微球在胃黏膜表面具有良好的黏附特性 ,且药物缓释可达 8h。

Preparation of trimebutine maleate gastric mucoadhesive microspheres by extrusion-spheronization method

Objective To prepare the trimebutine maleate gastric mucoadhesive microspheres by the method easy to be industrialized.Methods The microspheres were prepared by an extrude-spheronization method.The mucoadhesion was evaluated via counting the microspheres retaining on the gastric mucosa.In vitro the drug release was also studied.The factors influencing the mucoadhesion and the drug release such as thermal treatment,CP content,SA-CP/EC ratios,TM content,particle size were also studied respectively.Results While the CP content was increased,both the mucoadhesion and dug release rate of the microspheres increased.The more the TM content was,the worse the mucoadhesion was and the faster TM released.The mucoadhesion of the microspheres was also reduced when the particle size was increased and the release slowed.Both the retaining time in the stomach and the action intensity of the optimized formulation increased.Conclusion The microspheres had a good mucoadhesion and sustained release for 8h when the TM content was≤20%,the particle size was between 500～900 μm and the CP content was 13.30%.