INSILICO SCREENING OF COFORMERS, DEVOLPOMENT OF COCRYSTAL TO ENHANCE DISSOLUTION AND SOLUBILITY OF FAMOTIDINE
Parth Sarathi
Noida Institute of Engineering and Technology (Pharmacy Institute) , Plot 19, Knowledge Park 2, Greater Noida, Uttar Pradesh-201306, India, parthsarthigkp007@gmail.com
Mrs. Swarupanjali Padhi
Noida Institute of Engineering and Technology (Pharmacy Institute), Plot 19, Knowledge Park 2, Greater Noida, Uttar Pradesh-201306, India.
Mrs. Pragati Srivastava
Tahira Institute of medical science, Sector-7, GIDA, Gorakhpur, Uttar Pradesh – 273209, India
Abstract
The solubility and dissolution profile of the drug directly affects the therapeutic efficacy of the drug. Cocrystallization offers a promising method to improve the dissolution and solubility of the drug. Pharmaceutical cocrystals are multicomponent systems made of API and acceptable cocrystal formers in the same lattice. Cocrystals are increasingly popular in the pharmaceutical industry since extending the opportunity to improve the physicochemical property of drugs without affecting the internal activity of the compound. In this study famotidine, an antiulcer agent taken as a model drug. It is very slightly soluble in water, due to its low solubility categorized in BCS class 2. Here a very effective method of Insilico screening applied to the screening of coformers and cocrystal formation. The virtual screening technique, a computational tool developed the efficiency of screening the coformers to limited the coformer for experimentally study. Seven coformers from the GRAS list were screened with API. Binding affinity and the possibility of formation of H- bond interaction were computationally determined. Autodock was used for docking. Based on molecular docking citric acid ( Ei -2.6kcal/mol0 was selected as the best coformer. The work was continued by the cocrystallization process using the solvent evaporation method. Assay of solubility in water and dissolution at different pH like 2.5,3.5,6.4 was performed using UV spectrophotometric. Characterization of cocrystal was done by FTIR, DSC, Powder XRD. A morphological study was done by trinocular microscopy and SEM. The prepared cocrystal of famotidine- citric acid showed remarkable improvement in dissolution and solubility.
Keywords:
Molecular docking, Coformers, Famotidine,Cocrystal , Dissolution
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