ABSTRACT

A pharmaceutical salt is an ionizable drug presented in a neutral complex with a counterion. The hydrophobicity of the counterion and the melting point of the salt both play a role in the solubility of the salt form. Choosing an organic species to react with a drug to develop an organic salt has the potential to provide advantages including lower toxicities and, perhaps surprisingly, a higher aqueous solubility than an inorganic counterion can provide. Macromolecules and colloidal salt particles have a particular affinity for the lymphatic system and are returned to the vascular compartment through the thoracic duct. A microfluidization platform was proposed as a means to profoundly reduce the mass of drug employed in the study of salt formation and selection. The salt form will influence a number of physicochemical properties, which can then affect the availability and formulation characteristics of the drug.