Insulin Derivatives with Hydrophilic Side Chains for High Concentration Stability

The patent modifies the chemical structure of insulin by attaching side chains containing hydrophilic groups (such as carboxymethyl, hydroxyl, or amino groups) to the insulin molecule. This parameter change in the molecular structure increases water solubility, enabling the formulation to achieve high insulin concentrations (above 1.5 mM, preferably above 3 mM or 4 mM) without excessive viscosity or precipitation.

The patent introduces side chains with specific chemical properties (hydrophilic groups, specific molecular weights) to modify the physical parameters of insulin. These parameter changes stabilize the insulin formulation at high concentrations by preventing aggregation and maintaining a stable oligomerization pattern, thus improving physical stability while achieving high insulin concentration.

The patent modifies the chemical parameters of insulin by attaching side chains that protect the insulin molecule from degradation. These side chains can include groups that reduce susceptibility to proteolysis or oxidation, thereby improving chemical stability while maintaining high insulin concentration (above 1.5 mM) throughout the shelf life of the formulation.

The patent changes the molecular parameters of insulin by attaching hydrophilic side chains, which increase the hydrodynamic volume and improve solvation. This parameter change reduces intermolecular interactions that lead to viscosity increase, allowing the formulation to maintain lower viscosity even at high insulin concentrations (above 1.5 mM, preferably above 3 mM or 4 mM).