Preparation and Evaluation of Aripiprazole Oral Disintegrating Tablets / 中国药师

ABSTRACT

Objective:To prepare aripiprazole oral disintegrating tablets , investigate the formula and evaluate the quality .Meth-odsThe formula of aripiprazole oral disintegrating tablets was investigated by a factorial experiment design .The aripiprazole particle size distribution ( X1 , D90/μm) , the ratio of mannitol to microcrystalline cellulose ( X2 ,％) and the amount of disintegration ( X3 ,％) were selected as the independent variables , and the tablet hardness ( Y1 , N) , the disintegration time ( Y2 , s) and the dissolution in 30 min ( Y3 ,％) were used as the dependent variables to ultimately determine the optimal formula .The dissolution profile of aripiprazole oral disintegrating tablets and the reference preparation in four dissolution media were compared by f2 similarity factor, and the stability of aripiprazole oral disintegrating tablets was investigated by accelerated stability testing .Results: The results of factorial experiment design of variance analysis showed that the filler ratio had significant effect on the tablet hardness (P<0.05), the amount of disinte-grant and the filler ratio had significant effect on the disintegration time (P<0.05), and the aripiprazole particle size had significant effect on the drug dissolution ( P<0.05 ) .The optimal formula of aripiprazole oral disintegrating tablets was as follows the particle size D90 of aripiprazole was 20-40μm, the amount ratio of mannitol to microcrystalline cellulose was 2.51, and the amount of disinte-gration was 5.0％.Aripiprazole oral disintegrating tablets prepared with the optimal formula had higher hardness , shorter disintegration time and faster drug dissolution , and the dissolution profiles were similar with those of the reference preparation .The relevant sub-stances showed no significant increase during the accelerated stability testing , and the quality was satisfactory .Conclusion:The formu-la of aripiprazole oral disintegrating tablets is reasonable , the preparation process is feasible and the quality is controllable .