High-Sugar Glucagon Formulation for Pump Stability

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Solution Overview

Problem

Current glucagon formulations for treating hypoglycemia are chemically and physically unstable, leading to rapid degradation and gel formation, making them unsuitable for use in bi-hormonal pumps, which require a stable and pump-able solution for extended periods at body temperature.

Innovation Solution

A stable glucagon formulation is achieved by incorporating high concentrations of sugar (20% or more) to inhibit fibril formation and chemical degradation, creating a hypertonic solution that remains non-gelling and chemically stable for 3.5 to 7 days, suitable for use in insulin or bi-hormonal pumps.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If glucagon is formulated as a reconstituted solution with lactose monohydrate and sterile water, then it provides a dry environment for chemical stability, but the reconstituted solution becomes chemically and physically unstable and must be used immediately

Engineering Contradiction:
Improvechemical stabilityVSAvoidduration of stability
Core Design Contradiction:
Stability of the object's compositionVSDuration of action of stationary object

Solution Approach 1:

The patent changes the concentration parameter of sugar from conventional low levels to high concentrations (20% or more, preferably 40-70%). This parameter change fundamentally alters the solution properties, creating a hypertonic environment that prevents glucagon degradation and gel formation, thereby extending stability duration from immediate use to 3.5-7 days at body temperature

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite formulation combining glucagon with high concentrations of sugar (dextrose, sucrose, or other acceptable sugars). This composite system leverages the sugar's ability to form a protective matrix that stabilizes glucagon, preventing both chemical degradation and physical gelation while maintaining pumpability

Inventive Principle:
Principle #40Composite materials

2Ease of operation

If glucagon is delivered in small volumes through narrow-bore infusion tubing, then it enables pump delivery, but the solution must remain non-gelling and pump-able for extended periods

Engineering Contradiction:
ImprovepumpabilityVSAvoidduration of stability
Core Design Contradiction:
Ease of operationVSDuration of action of stationary object

Solution Approach 1:

The patent adjusts the viscosity and tonicity parameters by incorporating high sugar concentrations. This creates a hypertonic solution that maintains appropriate flow characteristics for pump delivery through narrow-bore tubing while preventing gel formation during extended storage at body temperature for 3.5-7 days

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent enables the use of disposable pump reservoirs containing pre-formulated stable glucagon solution. The formulation's stability allows these disposable components to be prepared in advance and used over extended periods, replacing the need for frequent manual preparation of unstable solutions

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Stability of the object's composition

If high concentrations of sugar (20% or more) are incorporated to inhibit fibril formation, then glucagon stability is maintained for 3.5 to 7 days, but the solution becomes hypertonic

Engineering Contradiction:
Improvechemical stabilityVSAvoidhypertonicity
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent converts the potentially harmful effect of hypertonicity into a beneficial stabilizing mechanism. The high sugar concentration creates a hypertonic environment that draws water into the solution, preventing glucagon from interacting with water molecules that would otherwise promote degradation and gel formation. The hypertonicity itself becomes the protective factor

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The high-sugar glucagon solution effectively prevents gelation and chemical degradation, maintaining glucagon stability and allowing for safe, prolonged use in pumps, enhancing the management of hypoglycemia by maintaining blood glucose levels.

Implementation Method 1

incorporating high concentrations of sugar (20% or more) to inhibit fibril formation and chemical degradation

Methodology Applied
Scientific EffectChemical degradation inhibition:

Implementation Method 2

high concentrations of sugar (20% or more) to inhibit fibril formation and chemical degradation, creating a hypertonic solution that remains non-gelling

Methodology Applied
Scientific EffectGelation prevention:

Data Source

PatentUS10238717B2Parenteral glucagon formulations
Publication Date: 2019.03.26 LATITUDE PHARMACEUTICALS INC

AI summary

This invention relates to compositions of glucagon suitable for administration by manual injection or by an insulin pump or other injection device to treat hypoglycemia. Said compositions comprise glucagon and a sugar, have a final pH between about 1.5 and 3, and are gel-free, chemically-stable at body temperature and pump-able.