Abstract

COCRYSTAL TECHNIQUE FOR THE IMPROVEMENT OF SOLUBILITY

Deepayan Kar*, Mousumi Das, Susmita Maiti, Nilanjan Adhikari, Biplab Kumar Chakra

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Abstract

Over 80% of the market’s formulations are solid dosage forms meant to be taken orally. 40% of these medications, associated with a comparable proportion of novel chemical entities, have poor water solubility, particularly those classified as BCS Class II and Class IV. Research and development of new products are also hampered by low oral bioavailability and poor water solubility, which may reduce the effectiveness of oral administration in patients. Co-Crystallization is one of the latest approaches which used for the enhancement of solubility of poorly aqueous soluble drugs also helps to improve physicochemical properties such as melting point, tabletability, solubility, stability, bioavailability and permeability with preserving the pharmacological properties of the active pharmaceutical ingredient. Cocrystals are multicomponent systems of two components, a coformer and an active medicinal ingredient, present in a stoichiometric ratio and bound together via π-π stacking interactions, hydrogen bonding, and Vander Waals forces. For the synthesis of cocrystals, a variety of techniques have been employed, including the Slurring Technique, Solution Methods, Colling Crystallization, Solution Crystallization, Grinding Method, Dry Grinding, Liquid Assisted Grinding, Anti-solvent Addition, Solvent Evaporation Method, Super Critical Fluid Technology, Spray Drying, and Hot Melt Extrusion Method. A comprehensive discussion of pharmaceutical cocrystals is provided in this article, along with information on how cocrystals differ from other methods of enhancing solubility, the difficulties in developing cocrystals, their use, and their prospects for the future.

Keywords: Cocrystal, Co-crystallization, Coformer, Bioavailability, Solubility, Stability.