Peptide Composition for CNS Injury via pH Buffering
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Solution Overview
Problem
Current therapeutic drugs for ischemic strokes face challenges such as significant side effects, potential risks, and insufficient therapeutic efficiency, while peptide drugs are limited by storage conditions and stability issues, necessitating improved compositions for treating central nervous system injuries.
Innovation Solution
A pharmaceutical composition comprising a peptide with the amino acid sequence YEKLLDTEI or its functional variants, combined with a pH adjusting agent like histidine/arginine buffer and a filler like trehalose, to enhance stability and delivery, specifically designed for treating central nervous system injuries and neurodegenerative diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If peptide drugs are used to treat central nervous system injuries, then therapeutic efficacy is improved, but storage stability deteriorates due to pH changes and degradation during high-temperature and long-term storage
Solution Approach 1:
The patent introduces pH adjusting agents (such as histidine, arginine, or their buffers) as intermediaries to mediate between the peptide drug and the storage environment. These agents maintain optimal pH levels during storage, preventing peptide degradation while preserving therapeutic efficacy. The pH adjusting agents act as a buffer system that protects the peptide from environmental stress without requiring complex storage conditions.
2Reliability
If peptide drugs are used to treat excitatory neurotoxicity, then therapeutic efficiency is improved, but side effects and potential risks increase compared to conventional drugs
Solution Approach 1:
The patent optimizes the peptide sequence parameters and formulation parameters to enhance therapeutic efficiency while reducing side effects. By modifying amino acid sequences (such as using YEKLLDTEI or its variants) and adjusting formulation parameters (pH, fillers, stabilizers), the peptide achieves better target specificity and reduced off-target effects compared to conventional drugs, thereby improving the therapeutic index.
3Reliability
If peptide drugs are used for treatment, then therapeutic effectiveness is improved, but transportation requirements become more stringent and complex
Solution Approach 1:
The patent creates a protective environment for the peptide drug by incorporating pH adjusting agents and stabilizers that maintain an optimal chemical environment during storage and transportation. This formulation approach effectively creates a stable, controlled environment within the pharmaceutical product itself, reducing the need for complex external temperature control and special transportation infrastructure.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition provides improved stability and efficacy by maintaining peptide conformation during storage, resisting environmental stress, and effectively reducing cerebral infarction volume in stroke models, with potential applications in treating ischemic strokes and other neurodegenerative conditions.
Implementation Method 1
a pH adjusting agent like histidine/arginine buffer
Implementation Method 2
combined with a pH adjusting agent like histidine/arginine buffer and a filler like trehalose, to enhance stability and delivery
Data Source
AI summary
There is provided in the present application a pharmaceutical composition comprising a peptide comprising the amino acid sequence of YEKLLDTEI (SEQ ID NO: 1) or a functional variant thereof, a pH adjusting agent, and a filler. The peptide is an active peptide for the treatment of a central nervous system injury. The present application also provides a pharmaceutical composition comprising a chimeric peptide comprising an active peptide and an internalization peptide, a pH adjusting agent, and a filler. The present application also provides medical use of a pharmaceutical composition comprising the active peptide or the chimeric peptide.