GLP-1/GIP Dual Agonist Composition With SNAC for Stable Absorption

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Solution Overview

Problem

Existing GLP-1 drugs for treating type 2 diabetes mellitus face challenges such as dose-dependent gastrointestinal adverse reactions and limited therapeutic effects, while GIP polypeptides in diabetic patients exhibit reduced incretin function, necessitating a stable formulation to enhance treatment efficacy and reduce adverse reactions.

Innovation Solution

A pharmaceutical composition comprising a GLP-1 analog and an absorption enhancer, such as N-(8-(2-hydroxybenzoyl)amino) caprylate (SNAC), to improve stability and absorption, potentially combined with GIP polypeptides, for enhanced glucose lowering and weight loss effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If the therapeutic dose of GLP-1 drugs is increased to achieve more remarkable treatment effects, then glucose lowering and weight loss effects are improved, but dose-dependent gastrointestinal adverse reactions occur more frequently

Engineering Contradiction:

Improvetherapeutic doseVSAvoidgastrointestinal adverse reactions

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent introduces an absorption enhancer as an intermediary substance that facilitates the absorption of GLP-1 drugs at lower doses. This mediator enables the drug to achieve therapeutic effects without requiring high doses that would trigger gastrointestinal adverse reactions, thus resolving the contradiction between dose quantity and harmful effects.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the absorption parameters of GLP-1 drugs by combining them with absorption enhancers. This parameter change allows the drug to be absorbed more efficiently at lower concentrations, achieving the same therapeutic effect without increasing the dose to levels that cause gastrointestinal side effects.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If GLP-1 drugs are used to treat type 2 diabetes mellitus, then therapeutic effects are achieved, but gastrointestinal adverse reactions occur

Engineering Contradiction:

Improvetherapeutic effectsVSAvoidgastrointestinal adverse reactions

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The absorption enhancer serves as a mediator that improves drug absorption efficiency, allowing therapeutic effects to be maintained or enhanced while using lower doses that do not trigger gastrointestinal adverse reactions.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

By changing the absorption parameters through combination with absorption enhancers, the patent maintains reliable therapeutic effects while operating in a dose range that avoids gastrointestinal side effects.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If chemically modified polypeptide drugs are administered, then therapeutic effects are enhanced, but stability during storage and use deteriorates

Engineering Contradiction:

Improvetherapeutic effectVSAvoidstability during storage and use

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent creates a composite pharmaceutical formulation by combining chemically modified polypeptide drugs with absorption enhancers and other excipients. This composite structure provides both the enhanced therapeutic effect of the modified polypeptide and the stability required for storage and use, with the absorption enhancer and formulation components protecting the polypeptide from degradation.

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS20260014232A1Pharmaceutical Composition of GLP-1 and GIP Receptor Dual Agonist and Use Thereof

Publication Date: 2026.01.15 JIANGSU HENGRUI MEDICINE CO LTD

AI summary

Provided are a pharmaceutical composition of GLP-1 and GIP receptor dual agonist and the use thereof. The pharmaceutical composition has good dissolution characteristics and stability.