Human Growth Hormone Liquid Formulation Stabilization

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Solution Overview

Problem

Current liquid formulations of human growth hormone suffer from instability, leading to deamidation and aggregation, which affects long-term storage stability and safety, despite efforts to improve convenience and stability through various buffer and surfactant combinations.

Innovation Solution

A stable liquid formulation is achieved by combining L-lysine or L-arginine as a stabilizer with poly(oxyethylene) poly(oxypropylene) copolymer or polyethylene glycol-15 polyoxystearate as a surfactant, enhancing the stability of human growth hormone by minimizing deamidation and aggregation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If human growth hormone is formulated in liquid form to improve convenience, then ease of operation is improved, but stability deteriorates due to deamidation and aggregation

Engineering Contradiction:
Improveconvenience of liquid formulationVSAvoidstability of human growth hormone
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent introduces L-lysine or L-arginine as intermediary substances that mediate between the human growth hormone and the aqueous environment. These amino acids act as stabilizers that prevent direct harmful interactions between water and the hormone, thereby maintaining stability while preserving the convenience of liquid formulation.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs simple, readily available amino acids (L-lysine or L-arginine) as stabilizing agents. These are inexpensive, easily incorporated substances that provide effective protection against degradation without requiring complex or expensive stabilizing systems.

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

2Reliability

If deamidation is prevented to maintain stability, then purity is improved, but this requires specific buffer conditions that may limit formulation flexibility

Engineering Contradiction:
Improvepurity of human growth hormoneVSAvoidformulation flexibility
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent utilizes changes in pH parameters through buffer systems to control the deamidation reaction. By adjusting and maintaining specific pH ranges, the formulation prevents deamidation while allowing flexibility in other formulation aspects. The addition of L-lysine or L-arginine further modulates the chemical environment to stabilize the hormone.

Inventive Principle:
Principle #35Parameter changes

3Object-affected harmful factors

If aggregation is minimized to ensure safety, then harmful factors are reduced, but this requires specific surfactant combinations that increase formulation complexity

Engineering Contradiction:
Improveaggregation of human growth hormoneVSAvoidcomplexity of surfactant combination
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent introduces non-ionic surfactants as intermediary substances that mediate between the human growth hormone molecules and the aqueous environment. These surfactants form protective interfaces that prevent direct protein-protein interactions leading to aggregation, while maintaining biocompatibility and safety.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Duration of action of stationary object

If long-term storage stability is improved through specific amino acid and surfactant combination, then reliability is improved, but manufacturing precision is required to achieve optimal stability

Engineering Contradiction:
Improvelong-term storage stabilityVSAvoidprecision of formulation preparation
Core Design Contradiction:
Duration of action of stationary objectVSManufacturing precision

Solution Approach 1:

The patent specifies optimal concentration ranges for L-lysine or L-arginine (0.01-1.0% w/v per mg of hGH) and non-ionic surfactants (0.01-1.0% w/v) to achieve maximum stability. By defining these parameter ranges, the formulation achieves long-term storage stability while providing guidance for manufacturing to ensure consistent quality without requiring excessive precision.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP2049148B1A stable liquid formulation of human growth hormone
Publication Date: 2016.09.28 DAEWOONG CO LTD
  • EP2049148B1 patent drawingFigure 1
  • EP2049148B1 patent drawingFigure 2

AI summary

Disclosed herein is a stable liquid formulation comprising human growth hormone; L-lysine, L-arginine or polyethylene glycol 300; and poly(oxyethylene) poly(oxypropylene) copolymer, polyethylene glycol- 15 polyoxystearate or polyethylene glycol-35 castor oil.