Stable GLP-1/GIP Dual-Receptor Agonist Composition

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Solution Overview

Problem

Current GLP-1/GIP receptor agonists face stability challenges due to degradation under various conditions, limiting their use in achieving maximum efficacy for treating type 2 diabetes mellitus.

Innovation Solution

A stable pharmaceutical composition of a GIP/GLP-1 dual-receptor agonist is developed, comprising an active polypeptide ingredient, a buffer solution, an osmotic pressure regulator, and a pH regulator, which enhances stability and efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high concentrations of GLP-1 RAs are used for long-term treatment, then blood glucose lowering and body weight reducing effects are maintained, but severe gastrointestinal side effects occur

Engineering Contradiction:

Improveblood glucose lowering effectVSAvoidgastrointestinal side effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the molecular structure of GLP-1 RAs by introducing specific amino acid substitutions and extensions (e.g., position 34 extension, position 26 substitutions) to create analogs with altered pharmacokinetic and pharmacodynamic properties that reduce gastrointestinal side effects while maintaining efficacy

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates composite peptide structures combining GLP-1 receptor agonist activity with modified amino acid sequences that include stabilizing elements and reduced immunogenicity, resulting in a composite molecule with improved tolerability profile

Inventive Principle:

Principle #40Composite materials

2Reliability

If the maximum dose of GLP-1 RAs is used to achieve potential maximum efficacy, then blood glucose control improves, but gastrointestinal side effects limit further dose increase

Engineering Contradiction:

Improveblood glucose controlVSAvoiddose tolerance

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent employs parameter changes in the peptide structure (amino acid sequence modifications, molecular weight adjustments) to shift the dose-response curve, allowing higher effective doses to be administered without proportionally increasing gastrointestinal side effects

Inventive Principle:

Principle #35Parameter changes

3Reliability

If GLP-1 RAs are administered to achieve significant body weight reduction, then metabolic effects improve, but gastrointestinal reactions increase

Engineering Contradiction:

Improvebody weight reducing effectVSAvoidgastrointestinal reactions

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent introduces parameter changes in the peptide structure including N-terminal extensions, C-terminal modifications, and internal amino acid substitutions to create analogs that selectively enhance body weight reduction effects while attenuating gastrointestinal adverse reactions

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20250170218A1Stable pharmaceutical composition of receptor agonist, and preparation method and application thereof

Publication Date: 2025.05.29 JIANGSU HANSOH PHARMA CO LTD

AI summary

The present invention relates to a stable pharmaceutical composition of a receptor agonist, a preparation method therefor and the use thereof. In particular, the present invention discloses a pharmaceutical composition having a dual-receptor agonist as an active ingredient. The pharmaceutical composition comprises a dual-receptor agonist buffer solution, an osmotic pressure regulator and a pH regulator. The pharmaceutical composition of the present invention has good drug stability and safety, and the preparation method is simple and convenient, and suitable for industrial production.