马来酸氟吡汀缓释片的研制及体外释放特性考察

目的：采用羟丙甲基纤维素（HPMC）作为亲水凝胶骨架材料,制备马来酸氟吡汀缓释片,并考察其体外释放特性。方法：通过单因素试验,分剐考察了HPMC、乳糖用量对马来酸氟吡汀缓释片释放速率的影响;以体外释放度为评价指标优选处方的最佳组成和比例。结果：马来酸氟吡汀缓释片的释放速度随处方中HPMC含量增加而减慢,随乳糖用量增多而加快;释放介质对马来酸氟吡汀的释放速率也有明显影响,而释放度测定方法、转速对马来酸氟吡汀缓释片的释放速率无明显影响。结论：本品处方组成合理,制备工艺稳定。制备的马来酸氟吡汀缓释片,体外释药曲线显示有明显的缓释作用,属于零级释放。

Preparation and in vitro Drug Release of Flupirtine Maleate Sustained Release Tablets

Objective：To prepare flupirtine maleate sustained-release tablets with once-daily dose using HPMC as the hydrophilic matrix material and investigate the release characteristics in vitro.Method：By single factor experiment,the effect of the amount of HPMC and lactose on release rate of the tablets was studied.The optimal formula was screened using the in vitro release as the index. Result：The drug release was decreased with the HPMC amount increase,and the release was increased with the lactose amount decrease.In addition,the medium showed significant influence on the release rate,while the assay method and stirring rate exhibited little effect on the release rate.Conclusion：The tablets with rational formula and stable preparation process have sustained release property and the release profile in vitro is fitted zero-order kinetics.