Osmotic Agents - Excipients Used in Parenteral Formulations of biotech Products

Osmotic Agents

For proteins the regular rules apply for adjusting the tonicity of parenteral products. Saline and mono- or disaccharide solutions are commonly used. These excipients may not be inert; they may influence protein structural stability. For example, sugars and polyhydric alcohols can stabilize the protein structure through the principle of “preferential exclusion” (Arakawa et al., 1991). These additives (water struc-ture promoters) enhance the interaction of the solvent with the protein and are themselves excluded from the protein surface layer; the protein is preferentially hydrated. This phenomenon can be monitored through an increased thermal stability of the protein. Unfortunately, a strong “preferential exclusion” effect enhances the tendency of proteins to self-associate.