SOLID DISPERSION TECHNIQUE TO ENHANCE THE SOLUBILITY AND DISSOLUTION RATE OF ARIPIPRAZOLE BY FUSION METHOD
Objective: The objective of the present study was to enhance the solubility and dissolution rate of Aripiprazole (APZ), a water insoluble drug, by a solid dispersion technique.
Methods: Solid dispersions (SD) of APZ were prepared by fusion method using water-soluble carriers like, polyethylene glycol 4000 (PEG 4000), Croscarmellose sodium (CCS) and Crospovidone (CP) and were characterized by in-vitro dissolution, Fourier transform infrared (FTIR) spectroscopy and Differential scanning calorimetry (DSC) studies.
Results: PEG 4000 physical mixtures containing APZ, showed enhanced dissolution rate as compared with pure drug. Binary solid dispersions showed an improvement in the dissolution rate when compared to the physical mixtures (PM) and pure drug. From ternary solid dispersions with CCS, formulation code SD9 showed 88.2% and with CP, formulation code SD15 showed 70.9%, whereas pure drug showed 18.8 % drug release at the end of 60 min. Based on the in-vitro dissolution studies of solid dispersions, the SD9 was selected to prepare tablets. From the dissolution studies of tablets, the formulation 4F3 showed rapid dissolution than other formulations and pure drug. FTIR, DSC studies suggesting that there was no physical and chemical interaction in between APZ and carriers.
Conclusion: Hence, it can be concluded that ternary solid dispersions in association with super disintegrants were more effective to increase the dissolution rate of low soluble drug than solid binary dispersions, physical mixtures, and pure drug.
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