GLP-1 Agonist Microsphere Suspension for Long-Term Injection Stability
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Solution Overview
Problem
Existing GLP-1 receptor agonists, GIP/GLP-1 receptor agonists, and GLP-1/GIP/GCG receptor triple agonists face issues with enzymatic degradation, insufficient absorption, and first-pass metabolism, necessitating daily injections and separate packaging of microspheres and aqueous carriers, which complicates administration and stability.
Innovation Solution
A pharmaceutical composition comprising microspheres containing GLP-1 receptor agonists, GIP/GLP-1 receptor agonists, or GLP-1/GIP/GCG receptor triple agonists, using fluid oils, surfactants, and polyhydric alcohols as carriers, with biocompatible polymers, and optionally additives, to enhance stability and bioavailability, allowing for long-term suspension and improved dissolution characteristics.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If microspheres are prepared with aqueous carriers, then the formulation can be administered as injection, but the microspheres do not have long-term stability and must be packaged and stored separately
Solution Approach 1:
The patent changes the carrier parameter from aqueous to non-aqueous (oil-based carriers including MCT oil, castor oil, cottonseed oil, sesame oil, or their mixtures). This parameter change enables long-term stability of microspheres in suspension without requiring separate packaging, directly resolving the contradiction between stability and complexity.
2Reliability
If daily injections are administered, then therapeutic effect is maintained, but patient convenience is reduced and administration frequency is high
Solution Approach 1:
The patent employs sustained-release microspheres that dynamically control drug release over extended periods (weeks to months). The oil-based carrier system enables controlled release kinetics, maintaining therapeutic effects while reducing injection frequency from daily to once-monthly or less, resolving the contradiction between therapeutic reliability and time loss.
3Reliability
If separate packaging of microspheres and carriers is used, then stability is maintained, but patient convenience is reduced due to multiple mixing steps
Solution Approach 1:
The patent merges the microspheres and oil-based carriers into a single stable suspension formulation. The microspheres are directly suspended in the oil carrier during manufacturing, creating a ready-to-administer single-phase product that eliminates the need for separate packaging and mixing steps, thereby resolving the contradiction between stability and ease of operation.
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 maintains long-term stability and bioavailability of the microspheres, reducing the frequency of injections and simplifying administration by ensuring precise drug concentration without separate mixing steps.
Implementation Method 1
microspheres containing one or more selected from a GLP-1 receptor agonist, a GIP/GLP-1 receptor agonist and a GLP-1/GIP/GCG receptor triple agonist; and one or more pharmaceutically acceptable first carriers selected from the group consisting of a fluid oil containing a fatty acid ester, a surfactant and a polyhydric alcohol
Data Source
Figure 1
AI summary
The present invention provides a pharmaceutical composition, comprising: microspheres containing one or more selected from a GLP-1 receptor agonist, a GIP/GLP-1 receptor agonist and a GLP-1/GIP/GCG receptor triple agonist; and one or more pharmaceutically acceptable first carriers selected from the group consisting of a fluid oil containing a fatty acid ester, a surfactant and a polyhydric alcohol. The microspheres of the pharmaceutical composition remain stable for a long period of time in a suspension formulation, and the microspheres stored for a long period of time exhibit excellent dissolution characteristics. In addition, the pharmaceutical composition exhibits the effects of increasing bioavailability and reducing the dosage to be administered.