Glutamic Acid Peptide Formulation Stability

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Solution Overview

Problem

Current treatments for obesity-related conditions such as diabetes and non-alcoholic fatty liver disease lack effective pharmaceutical solutions, particularly for sustained release formulations that prevent peptide gelling and maintain stability at various temperatures.

Innovation Solution

A formulation comprising glutamic acid and a peptide, specifically MOTS-c or its analogs, which are stable for extended periods, prevent gelling, and can be administered through standard needles, with a pH range of 3-7 and concentrations of 25-75 mg/mL, ensuring effective delivery and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If peptide formulations are used to treat obesity-related conditions, then therapeutic effectiveness is improved, but peptide gelling and instability occur

Engineering Contradiction:

Improvepeptide stabilityVSAvoidgelling

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent introduces glutamic acid as an intermediary substance that mediates between the peptide and the formulation environment. Glutamic acid acts as a stabilizing agent that prevents peptide gelling while maintaining therapeutic effectiveness, resolving the contradiction between reliability and harmful gelling effects

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies formulation parameters by incorporating glutamic acid at specific concentrations and adjusting pH levels. These parameter changes transform the formulation from an unstable, gelling-prone state to a stable, sustained-release formulation that maintains peptide effectiveness

Inventive Principle:

Principle #35Parameter changes

2Duration of action of moving object

If sustained release formulation is developed, then treatment duration is improved, but formulation stability is compromised

Engineering Contradiction:

Improvesustained release durationVSAvoidformulation stability

Core Design Contradiction:

Duration of action of moving objectVSStability of the object's composition

Solution Approach 1:

The patent ensures continuous useful action by formulating a sustained-release composition that maintains stable peptide delivery over extended periods. The glutamic acid-containing formulation prevents gelling and maintains composition stability throughout the entire duration of action, eliminating the trade-off between duration and stability

Inventive Principle:

Principle #20Continuity of useful action

3Quantity of substance

If peptide concentration is increased for effective delivery, then therapeutic effect is improved, but gelling tendency increases

Engineering Contradiction:

Improvepeptide concentrationVSAvoidgelling tendency

Core Design Contradiction:

Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

Glutamic acid serves as a mediating substance that allows high peptide concentrations to be maintained without triggering gelling. The intermediary glutamic acid decouples the relationship between concentration and gelling tendency, enabling effective therapeutic levels while preventing harmful aggregation

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS11517608B2Peptide-containing formulations

Publication Date: 2022.12.06 COHBAR

AI summary

A formulation comprising glutamic acid, or a salt thereof, and an effective amount of a peptide is provided. The invention also provides a method of preparing the formulation, methods of treating a condition using the formulation, and a kit containing components of the formulation. The invention further provides a sustained release formulation for drug substances comprising glutamic acid, or a salt thereof, and an amount of a peptide.