Antioxidant Dipeptide Composition for Stable Lyophilized Injection

The patent extracts the active dipeptide derivative from the oral dosage form and formulates it as an injectable preparation, thereby removing the harmful enzymatic environment of the gastrointestinal tract while maintaining drug delivery. This resolves the contradiction by eliminating the source of degradation (enzymes in oral cavity) while preserving administration effectiveness through injection.

The patent introduces protective excipients and specific formulation components as intermediaries that shield the dipeptide derivative from enzymatic degradation. These intermediaries create a protective microenvironment that prevents enzyme-substrate interaction, allowing the drug to maintain efficacy while being administered in a form that can withstand the gastrointestinal environment or be delivered parenterally.

The patent changes the physical and chemical parameters of the formulation by adjusting pH to specific ranges (6.0-8.0), controlling ionic strength, and optimizing temperature conditions during storage and sterilization. These parameter changes create optimal conditions for drug stability while maintaining usability, allowing the formulation to withstand moist heat sterilization without degradation.

The patent creates a composite formulation system combining the dipeptide derivative with multiple excipients including buffering agents, stabilizers, and protective compounds. This composite material approach provides synergistic protection where each component contributes to overall stability, enabling the formulation to resist degradation during storage and sterilization while remaining easy to administer.

The patent creates a highly stable formulation copy that replicates the therapeutic effect at optimized concentrations. By improving formulation stability through excipients and pH control, the patent enables maintenance of higher drug concentrations without proportional increase in impurities, as the stable formulation prevents degradation-related impurity formation.

The patent optimizes concentration parameters within specific ranges (0.5-10.0 mg/mL) and combines this with controlled pH (6.0-8.0) and ionic strength parameters. These parameter optimizations allow achieving high treatment efficiency while minimizing impurity generation, as the controlled parameters prevent degradation reactions that would otherwise produce harmful impurities even at high concentrations.