European Journal of Biomedical and Pharmaceutical Sciences

SOLUBILITY ENHANCEMENT OF RISPERIDONE BY COCRYSTALLISATION TECHNIQUE

Viresh K. Chandur*, Paul George and A. R. Shabaraya

ABSTRACT

Solubility is a major parameter for the absorption process of a drug. Therefore, increasing the dissolution rate of poorly water-soluble drug is important in enhancing their bioavailability. The present study is aimed to increase solubility of Risperidone (RIS) by preparing cocrystals via cocrystallization technique using various coformers. The selection of coformers were according to the Hansen Solubility Parameters (HSP) and pKa screening methods. The coformers used in the present study are Benzoic acid, Benzamide, Aspirin, Piperazine and Benzamide. The cocrystals were prepared by solvent evaporation technique in which drug and coformer were dissolved in 1:3 molar ratio in a suitable solvent. The 1:3 ratio were selected based on the hydrogen bond donors and acceptors present in the parent drug and the coformers. The prepared cocrystals were preliminarily screened for its solubility and dissolution. Among the prepared cocrystals, RIS- Benzamide, RIS-Piperazine, RIS-Benzamide showed the best solubility and better dissolution rate. Further these three cocrystals were characterized with the help of advanced instrumental techniques such as FTIR, PXRD, DSC, and SEM. Thus, it was confirmed that the successfully prepared RIS-Benzamide cocrystals had shown a tremendous enhancement in their solubility than the API, which was higher when compared to marketed product and all other prepared cocrystals. It was concluded that cocrystallization method can be successfully used for improving the solubility of poorly soluble drugs.

Keywords: Cocrystal, Coformer, Hydrogen Bonding, Hansen Solubility Parameter, pKa Screening.