European Journal of Molecular & Clinical Medicine

Abstract

Aripiprazole is a bitter drug, freely soluble in organic solvents but it is practically insoluble in water & its solubility is pH dependent. Therefore, In order to ensure adequate bioavailability, aripiprazole and betacyclodextrine are subjected to three different weight ratios (B5 1:1, 1:1.5, and 1:2).ARP-BCD complexes, are prepared by solid dispersion technique to improve dissolution & bioavailability of this poorly water soluble drug. Batch B5 (ii), in which the drug was complexed with β-Cyclodextrin in the ratio (1:1.5) shows 100% drug release within 60 minutes &  it releases above 90% drug within 10 minutes .Wet granulation technique was implemented to compressed tablets of best resulted ARP-BCD complex B5 1:1.5( B6), Finally the compressed tablets were evaluated for their different parameter, like, crushing strength, friability, disintegration time, and dissolution, In vivo disintegration time, Bitterness Index, resulted a successful formulation. .Batch B6 (iv) the combination of MCC (ceolus KG 802) & xylitol as a filler shows best disintegration characteristics, acceptable friability, good mouth feel, sufficient hardness and 100% dissolution profile. To the optimized batch of B6 (iv)  Acesulfame potassium ,and other sweetners and flavours were added. The intensity of the bitterness was found out by comparing the bitter index level of prepared 3 batches i.e. X1, X2, and X3. .Batch X3 with 2% sweetening & flavouring agent produces tasteless tablets with good & pleasant mouthfeel.So it was concluded that by means of addition of 2% of sweetening & flavouring agent the bitter taste masking was achieved upto the required level.