Speaker
Description
Most of the new chemical entities (NCEs) that are being developed suffers from poor physicochemical properties like low solubility, low permeability which in turn results in poor and erratic bioavailability. In order to improve the poor physicochemical properties of the active pharmaceutical ingredients (API’s), various approaches like salt formation, particle size reduction, the addition of surfactant and co-solvent, amorphous solid dispersion, lipid-based formulation are available. Crystal engineering is an alternative approach to modify the physicochemical properties of the API’s, without changing its biological properties/inherent properties as cocrystals are produced by the supramolecular synthons which are formed by non-covalent bonds like H-bonding, Van-der Waal’s interaction, π-interactions between the API and the coformer. The result of the formation of these supramolecular synthons is the formation of a multiple-component crystal such as cocrystals, hydrates or solvates. Pharmaceutical cocrystals are a subset of the multicomponent crystal where one component is an Active Pharmaceutical Ingredient (API) and the second one (Coformer) is selected from Generally Regarded as Safe (GRAS) list without any disruption of the covalent bonds of the APIs and thus keeping the chemical structure intact. Pharmaceutical Cocrystals have shown significant impact in altering the physicochemical properties of the APIs which in turn leads to an increase in the bioavailability of it.
Keywords: Crystal engineering, physicochemical properties, low solubility, bioavailability