卡维地洛微孔渗透泵颗粒的制备及其性能

目的:制备卡维地洛微孔渗透泵颗粒,并对其性能进行研究。方法:以卡维地洛作为模型药物,以氯化钠为渗透压活性物质,酒石酸为溶解度调节剂,醋酸纤维素为包衣膜材,PEG400为水溶性致孔剂,采用正交试验设计法L9(34)优选卡维地洛微孔渗透泵颗粒制备工艺。结果:卡维地洛微孔渗透泵颗粒在模拟胃肠环境中按零级动力学方式释放药物,具有明显的渗透泵特征和控释效果,且基本不受胃肠pH环境的影响,12 h内累积释放度可达71.90%。结论:卡维地洛微孔渗透泵颗粒处方组成合理、制备工艺可行,可望成为一种新的卡维地洛控释剂型。

Study on preparation and properties of the microbore osmotic pump granules loaded carvedilol

OBJECTIVE To prepare carvedilol microbore porosity osmotic pump granules,and study its properties.METHODS Using carvedilol as a model drug,NaCl as the osmotic active agent,tartaric acid as the solubility regulator,cellulose acetate as the coating materials,and PEG 400 as the water-soluble pore-forming agent,the carvedilol microbore osmotic pump granules technology were optimized by orthogonal design of L9(34).Also,its some properties were studied.RESULTS The deliveries of carvedilol microbore osmotic pump granules was found to accord with a zero order rate in the simulated gastro-intestinal tract environments,and no significant difference existed in the two kinds of pH conditions,the accumulated release achieved to 71.90% within 12 h.The carvedilol microbore osmotic pump granules possessed obviously osmotic pump feature and controlled release effect in vitro.CONCLUSION The preparing compositions of the carvedilol microbore osmotic pump granules were reasonable,and the preparation can be carried out.The carvedilol microbore osmotic pump granules have the potential to be a novel controlled release dosage form.