GLP-1R Agonist Formulation for Joint Disease Injection
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Solution Overview
Problem
Current pharmaceutical compositions for treating joint diseases, such as osteoarthritis, via intraarticular injection have limited duration of effect, requiring frequent injections and increasing patient discomfort and medical intervention.
Innovation Solution
A pharmaceutical composition comprising a GLP-1R agonist, a tromethamine or phosphate buffer, and an isotonic agent like glucose, polyethylene glycol, or propylene glycol, administered as a solution or suspension via intraarticular injection, providing a long-term effect lasting at least three weeks.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If current pharmaceutical compositions are administered via intraarticular injection, then the treatment effect is achieved, but the duration of effect is limited requiring frequent injections
Solution Approach 1:
The patent changes the chemical parameters of the pharmaceutical composition by selecting specific GLP-1R agonists with appropriate molecular properties and combining them with particular excipients (buffers like tromethamine or phosphate, and isotonic agents like glucose, polyethylene glycol, propylene glycol, or glycerol). These parameter changes in composition enable the formulation to maintain therapeutic efficacy for at least 3 weeks after a single intraarticular injection, thereby reducing injection frequency while maintaining treatment effectiveness.
2Ease of operation
If injection frequency is reduced to improve patient comfort, then patient comfort improves, but the duration of therapeutic effect must be extended
Solution Approach 1:
The patent modifies the pharmaceutical composition parameters by selecting specific buffers (tromethamine buffer or phosphate buffer) and isotonic agents (glucose, polyethylene glycol, propylene glycol, or glycerol) in optimized concentrations. These parameter changes ensure the formulation provides sustained release and maintains therapeutic effect for at least 3 weeks, thereby reducing injection frequency from weekly to monthly or less frequent, significantly improving patient comfort while maintaining efficacy.
3Duration of action of moving object
If the formulation is changed to extend duration of action, then the duration of effect increases, but the formulation complexity increases
Solution Approach 1:
The patent achieves extended duration of action (at least 3 weeks) by optimizing parameters within a relatively simple formulation structure: a GLP-1R agonist combined with standard pharmaceutical excipients (buffer and isotonic agent). The complexity is managed by selecting from established excipient categories rather than introducing complex delivery systems, maintaining formulation simplicity while achieving the desired prolonged effect through careful parameter selection and optimization.
Data Source
AI summary
The present invention relates to a pharmaceutical composition comprising a GLP-1R agonist such as liraglutide or semaglutide, a buffer selected from a tromethamine buffer and a phosphate buffer, and an isotonic agent selected from glucose, a polyethylene glycol and glycerol. The present invention also relates to said pharmaceutical composition for use in a method for treating joint diseases.