Teduglutide Stability via Sodium Ion Stabilization

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Solution Overview

Problem

Peptide formulations, such as teduglutide, face challenges in stability due to degradation, requiring special storage conditions and limited shelf life, making it difficult to maintain physical and chemical integrity during storage and administration.

Innovation Solution

Incorporating sodium ions in a stable injectable composition with pharmaceutically acceptable excipients enhances the stability of teduglutide, improving its physical stability and compatibility for longer-term storage and use.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If teduglutide is formulated as liquid for injection, then administration is convenient, but stability deteriorates due to degradation and physical changes during shelf life

Engineering Contradiction:
Improveease of administrationVSAvoidstability during shelf life
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent changes the chemical composition parameters by incorporating sodium ions (0.1-5.0% w/v) and specific excipients into the liquid formulation. This parameter modification stabilizes the peptide structure, preventing degradation and physical changes while maintaining liquid form for convenient administration.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces sodium ions and excipients as intermediary substances that mediate between the peptide and the formulation environment. These intermediaries protect the peptide from degradation by stabilizing its structure and preventing harmful interactions, thereby extending shelf life while maintaining liquid formulation benefits.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Stability of the object's composition

If sodium is added to enhance stability, then shelf life extends, but sodium content increases which may affect patients with sodium restrictions

Engineering Contradiction:
Improvestability and shelf lifeVSAvoidsodium content
Core Design Contradiction:
Stability of the object's compositionVSQuantity of substance

Solution Approach 1:

The patent optimizes the sodium concentration parameter to a specific range (0.1-5.0% w/v) that provides sufficient stability enhancement while minimizing excessive sodium content. This parameter optimization balances the conflicting requirements of stability and sodium content control.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies sodium ions locally as a stabilizing agent within the formulation rather than using high concentrations throughout. By strategically incorporating sodium at optimized levels alongside specific excipients, the formulation achieves local stabilization effect while controlling overall sodium content to acceptable levels for most patients.

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS20240415933A1Stable injectable compositions of GLP-2 peptide
Publication Date: 2024.12.19 ORBICULAR PHARMA TECH PTE LTD

AI summary

The present invention relates to a stable GLP-2 peptide injectable composition, comprising GLP-2 peptide agent comprises of sodium; wherein the GLP-2 peptide agent is teduglutide or h[Gly2]GLP-2 and one or more pharmaceutically acceptable excipient(s).