Dual GLP-1/GIP Agonist Composition for Preservative-Free Stability

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Solution Overview

Problem

Existing dual GLP-1 and GIP receptor agonist polypeptide-based drugs face issues with chemical degradation, polymerization, and the need for antimicrobial agents, which affect stability and safety, especially in liquid preparations at physiological pH.

Innovation Solution

A pharmaceutical composition comprising a dual GLP-1 and GIP receptor agonist with propylene glycol as a stabilizer and disodium hydrogen phosphate dodecahydrate as a buffer salt, maintaining a pH of 7.2-8.2, without antimicrobial agents, to ensure stability and solubility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If antimicrobial agents are added to polypeptide-based drug preparations, then product stability is improved, but drug safety is worsened due to direct circulation upon injection

Engineering Contradiction:

Improveproduct stabilityVSAvoiddrug safety

Core Design Contradiction:

Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent removes antimicrobial agents from the formulation entirely, extracting the harmful element while maintaining product stability through alternative means (proper pH control, stabilizers, and buffer salts). This eliminates the safety risk associated with preservatives that directly circulate upon injection.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent introduces stabilizers and buffer salts as intermediary substances that mediate between the polypeptide drug and the external environment. These intermediaries prevent degradation and microbial growth without requiring toxic antimicrobial agents, thus maintaining stability while ensuring safety.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If polypeptide-based drugs are formulated at physiological pH (7-8), then biological activity is maintained, but susceptibility to microorganial degradation increases

Engineering Contradiction:

Improvebiological activityVSAvoidsusceptibility to degradation

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent optimizes the pH parameter to a specific range (7.2-8.2) and uses buffer salts to maintain this parameter consistently. This parameter change and control creates an environment that supports biological activity while reducing microbial degradation susceptibility through proper pH control.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

Buffer salts act as intermediaries that stabilize the pH environment around the polypeptide drug. This intermediary substance maintains the physiological pH needed for biological activity while simultaneously creating conditions less favorable for microbial degradation.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Quantity of substance

If polypeptide-based drugs are prepared into liquid preparations, then solubility is improved, but polymerization and chemical degradation occur

Engineering Contradiction:

ImprovesolubilityVSAvoidpolymerization and degradation

Core Design Contradiction:

Quantity of substanceVSStability of the object's composition

Solution Approach 1:

Stabilizers and buffer salts serve as intermediary substances in the liquid formulation that prevent polymerization and chemical degradation. These intermediaries interact with the polypeptide molecules to maintain their structural integrity in the liquid state, ensuring solubility without compromising stability.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent controls key formulation parameters including pH, temperature, and concentration to prevent polymerization and degradation. By optimizing these parameters and using stabilizers, the patent achieves high solubility in liquid preparation while maintaining chemical stability and preventing unwanted reactions.

Inventive Principle:

Principle #35Parameter changes

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 the structural integrity and biological activity of the dual receptor agonist, preventing polymerization and degradation, allowing for long-term preservation and effective treatment of metabolic disorders like diabetes and obesity.

Implementation Method 1

a stabilizer, and a buffer salt; wherein the dual GLP-1 and GIP receptor agonist is a compound represented by formula I

Methodology Applied

Scientific EffectStabilization:

Implementation Method 2

disodium hydrogen phosphate dodecahydrate as a buffer salt, maintaining a pH of 7.2-8.2

Methodology Applied

Scientific EffectBuffering:

Implementation Method 3

the main function of the side chain is to bind to albumin (albumin having basic residues) in the blood, thereby extending the half-life

Methodology Applied

Scientific EffectBinding:

Data Source

PatentUS20260103497A1Dual GLP-1 and GIP receptor agonist pharmaceutical composition and use thereof

Publication Date: 2026.04.16 BRIGHTGENE BIO MEDICAL TECHNOLOGY CO LTD

AI summary

The present disclosure provides a dual GLP-1 and GIP receptor agonist pharmaceutical composition, comprising a dual GLP-1 and GIP receptor agonist, a stabilizer and a buffer salt. The present disclosure also provides use of the pharmaceutical composition in the preparation of a drug for preventing and/or treating metabolic disorder related diseases.