IgG Stabilization via Low pH and Glycine Formulation

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Solution Overview

Problem

There is a need for stable and well-tolerated intravenous immunoglobulin G (IgG) formulations that can withstand storage conditions without forming aggregates or undergoing physicochemical degradations, as high demand has led to supply tensions and safety concerns such as anaphylactic reactions and reduced blood pressure.

Innovation Solution

A pharmaceutical composition of human immunoglobulin G formulated with glycine and a non-ionic detergent at a pH between 4.4 and 4.8, specifically using polysorbate 80, which provides stability by reducing aggregate formation and chemical modifications, and can be in liquid or lyophilized form.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If conventional stabilizers (sugars, amino acids, mannitol) are added to IgG compositions, then stability during storage is improved, but formulation complexity and potential adverse reactions increase

Engineering Contradiction:
Improvestability during storageVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent changes the pH parameter to a low range (4.4-4.8) and maintains specific ionic strength conditions to achieve stabilization of IgG without requiring multiple conventional stabilizers. This parameter change allows the use of a simplified formulation containing only glycine and non-ionic detergent as stabilizing agents.

Inventive Principle:
Principle #35Parameter changes

2Duration of action of stationary object

If IgG is stored for extended periods, then supply availability is improved, but aggregate formation and physicochemical degradation increase

Engineering Contradiction:
Improvestorage durationVSAvoidaggregate formation
Core Design Contradiction:
Duration of action of stationary objectVSStability of the object's composition

Solution Approach 1:

By establishing specific pH (4.4-4.8) and ionic strength parameters in the formulation, the patent prevents aggregate formation and physicochemical degradation during extended storage periods, enabling long-term stability without compromise to composition integrity.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses glycine and non-ionic detergent as intermediary stabilizing agents that prevent direct interaction between IgG molecules that would lead to aggregation, thereby maintaining stability during long-term storage.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Stability of the object's composition

If stabilizing compounds are added to prevent degradation, then chemical stability is improved, but tolerance and safety profile may worsen

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

Solution Approach 1:

The patent uses pH and ionic strength as controlling parameters to achieve chemical stability through prevention of oxidation and hydrolysis reactions, rather than relying on multiple chemical stabilizers that could increase adverse reaction risk.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent extracts or removes the need for multiple conventional stabilizers (sugars, amino acids, mannitol) by using a simplified approach based on pH and ionic strength control, thereby reducing the number of components that could potentially cause adverse reactions.

Inventive Principle:
Principle #2Taking out (Extraction)

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 composition achieves enhanced physical and chemical stability, reducing the risk of adverse reactions and maintaining efficacy over extended storage periods, as demonstrated by stability tests showing comparable or superior performance to existing formulations without mannitol.

Implementation Method 1

The Applicant has now developed a pharmaceutical composition comprising human immunoglobulin G formulated with glycine and a non-ionic detergent, at a pH less than or equal to 4.8. The inventors have particularly demonstrated the importance of a low pH to stabilize this formulation.

Methodology Applied
Scientific EffectpH-dependent stabilization:

Implementation Method 2

A pharmaceutical composition of human immunoglobulin G formulated with glycine and a non-ionic detergent, at a pH between 4.4 and 4.8, specifically using polysorbate 80, which provides stability by reducing aggregate formation and chemical modifications

Methodology Applied
Scientific EffectSurfactant action: Surfactant

Implementation Method 3

A pharmaceutical composition comprising human immunoglobulin G (IgG), according to claim 1. The composition has a pH between 4.4 and 4.8. The composition according to the invention is advantageously in liquid form.

Methodology Applied
Scientific EffectStabilizer effect: Preservative

Data Source

PatentEP2582394B1Stabilised human immunoglobulin composition
Publication Date: 2019.10.23 LABE FR DU FRACTIONNEMENT & DES BIOTECH SA
  • EP2582394B1 patent drawingFigure 1A~2
  • EP2582394B1 patent drawingFigure 3

AI summary

The invention relates to a liquid pharmaceutical composition including human immunoglobulin G (IgG), including at least 200 mM, preferably 250 mM +/- 50 mM, of glycine and 20 to 100 mg/l of a non-ionic detergent, and having a pH of less than or equal to 4.8.