GLP-2 Peptide Injection Pen Lipid Depot Formulation

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current GLP-2 analogues for treating intestinal disorders require frequent administration due to their short plasma half-life, leading to patient discomfort and reduced compliance.

Innovation Solution

Development of GLP-2 analogues with a significantly longer terminal plasma half-life of 5 to 17 days, allowing for less frequent dosing, such as once or twice weekly, through the formation of a subcutaneous depot and slowly released metabolites.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If GLP-2 analogues are administered frequently to maintain therapeutic effect, then treatment efficacy is improved, but patient compliance deteriorates due to injection burden

Engineering Contradiction:
Improvetreatment efficacyVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent applies preliminary action by formulating the GLP-2 analogue in a lipid composition that creates a depot effect at the injection site. This preliminary formulation action ensures slow release of the peptide over time, maintaining therapeutic levels without requiring frequent re-injection, thus resolving the contradiction between treatment efficacy and patient compliance

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent uses lipid molecules as an intermediary substance between the GLP-2 analogue and the body's clearance mechanisms. The lipid composition acts as a mediator that binds to the peptide, protecting it from rapid degradation and enabling sustained release, thereby maintaining efficacy while reducing injection frequency

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If GLP-2 analogues are administered frequently to maintain therapeutic effect, then plasma concentration is maintained, but treatment complexity increases

Engineering Contradiction:
Improveplasma concentration maintenanceVSAvoiddosing regimen complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent achieves continuity of useful action through the lipid formulation that creates sustained release kinetics. The GLP-2 analogue is continuously released from the lipid depot over an extended period, maintaining stable plasma concentrations without the need for multiple discrete dosing events, thus simplifying the dosing regimen while maintaining therapeutic levels

Inventive Principle:
Principle #20Continuity of useful action

3Duration of action of moving object

If native hGLP-2 is used for treatment, then biological potency is maintained, but half-life is too short for clinical utility

Engineering Contradiction:
Improvehalf-lifeVSAvoidbiological potency
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent applies parameter changes by modifying the pharmacokinetic parameters of GLP-2 through lipid conjugation or lipid formulation. This changes the half-life parameter from minutes to days, while the lipid component is selected to not interfere with the peptide's biological activity, thus extending duration of action while maintaining potency

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses composite materials by combining the GLP-2 peptide with lipid molecules in a specific formulation. This composite structure allows the peptide to retain its biological potency while the lipid component provides extended circulation time and reduced clearance, achieving both long half-life and maintained efficacy

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS12297251B1Injection pen for subcutaneous administration of a peptide
Publication Date: 2025.05.13 ZEALAND PHARMA AS

AI summary

The invention features injection pens for the subcutaneous injection of a peptide and methods of using same.