Preparation of flupirtine maleate sustained release dropping pills

GU Cai-hong; L(U) Xiao-min; WANG Dong-dong; SUN Cheng; ZHANG Hui-kao; HU Rong

Abstract：Objective:To prepare flupirtine maleate sustained release dropping pills.Methods:Flupirtine maleate sustained release dropping pills were composed of two parts,which were prepared by solid dispersion technique using PEG6000 and stearic acid as the carrier materials.The similar factor method was used to compare the in vitro dissolution profiles of the sustained release dropping pills with the existing sustained release tablets.The mean cumulative release data were fitted to zero-order,first-order and Higuichi equations,respectively.Accelerated test and long-term test were used to investigate the stability.Results:The sustained-release dropping pills consisted of sustained-release and immediate-release parts at a ratio of 3∶ 1.The in vitro release percentages were 90％ and 30％ at 12 min for the two parts,respectively.The drug release time of the self-made flupirtine maleate sustainedrelease dropping pills was shorter,the flat top time of the dissolution curve was longer and the release rate was higher than that of the same dosage of the commercial sustained release tablets.The value of similarity factor f2 by calculating the data of dissolution test was 65,and the in vitro drug release profile of the self-made flupirtine maleate sustained release dropping pills was consistent with first-order release model.Flupirtine maleate and its sustained release dropping pills had good stability at 40 ℃ when sealed and could be stored for a long time at room temperature.Conclusion:The self-made sustained release dropping pills of flupirtine maleate have good property of sustained release in vitro which can reach effective plasma concentration quickly and release drugs over a longer period of time.The new formulation of dropping pills is worthy of further research.