Self-Invertible Emulsion Thickener for Pharmaceutical Formulations

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Solution Overview

Problem

Current pharmaceutical formulations rely on petrochemical-derived materials for thickening polar phases, which are unsustainable and inefficient, with existing biobased alternatives struggling to achieve high polymer content and effective thickening properties in aqueous media.

Innovation Solution

A pharmaceutical composition featuring a self-invertible water-in-oil emulsion with a polymer composition comprising partially or totally salified glutamic acid monomer units and a crosslinking agent bearing glycidyl functions, achieving a polymer content of at least 20% and providing enhanced thickening properties in aqueous media.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If biobased polymers are used as thickening agents, then environmental sustainability is improved, but thickening efficiency and polymer content are insufficient

Engineering Contradiction:
Improveenvironmental sustainabilityVSAvoidthickening efficiency
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent changes the molecular structure parameters of biobased polymers by introducing crosslinking points through glycidyl groups from epoxy compounds. This transforms linear polymer chains into three-dimensional networks, fundamentally altering the rheological properties and thickening capability of the biobased polymer in aqueous media

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite system combining biobased polymers (polyglutamic acid) with synthetic crosslinking agents (epoxy compounds). This hybrid approach leverages the environmental benefits of biobased materials while incorporating the effective crosslinking mechanism of synthetic agents to achieve superior thickening performance

Inventive Principle:
Principle #40Composite materials

2Reliability

If crosslinking reactions are performed to increase polymer branching, then thickening properties are improved, but manufacturing complexity increases

Engineering Contradiction:
Improvethickening propertiesVSAvoidmanufacturing complexity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent performs crosslinking reactions during the polymerization process itself, rather than as a separate post-processing step. The epoxy compounds are introduced into the reaction mixture, allowing crosslinking to occur concurrently with polymer chain formation, thereby simplifying the overall manufacturing process

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent optimizes reaction parameters including pH control (maintaining pH 2-3 during crosslinking), temperature, and the molar ratio of epoxy compounds to monomers. These parameter optimizations enable effective crosslinking under controlled conditions that do not significantly complicate the manufacturing process

Inventive Principle:
Principle #35Parameter changes

3Reliability

If high polymer content is achieved in aqueous media, then thickening effectiveness is improved, but formulation stability deteriorates

Engineering Contradiction:
Improvethickening effectivenessVSAvoidformulation stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent creates a composite network structure where crosslinked polyglutamic acid forms a three-dimensional matrix in aqueous media. This network structure prevents polymer aggregation and phase separation, maintaining formulation stability even at high polymer concentrations where conventional biobased polymers would fail

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The crosslinked regions create localized three-dimensional networks within the aqueous phase, providing stable thickening zones that prevent global formulation instability. The crosslinking creates micro-environments that maintain polymer solubility and distribution even at high overall concentrations

Inventive Principle:
Principle #3Local quality

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 effectively thickens polar phases, offering improved stability and viscosity, while being environmentally friendly and sustainable, addressing the limitations of existing biobased solutions.

Implementation Method 1

a pharmaceutical composition (F) comprising at least one pharmaceutical active principle and, as thickener, a composition (CA) in the form of an emulsion of the self-invertible water-in-oil type

Methodology Applied
Scientific EffectThickening:

Implementation Method 2

a composition (CA) in the form of an emulsion of the self-invertible water-in-oil type

Methodology Applied
Scientific EffectEmulsion: Emulsion

Implementation Method 3

synthetic polymers have the property of being deployed, in the polar phase, under the effect of electrostatic repulsions due to the presence of charges (negative and/or positive) on the linear or branched, crosslinked or noncrosslinked polymer backbone

Methodology Applied
Scientific EffectElectrostatic repulsion: Ion Repulsion/Attraction

Implementation Method 4

a polymer composition comprising partially or totally salified glutamic acid monomer units and a crosslinking agent bearing glycidyl functions

Methodology Applied
Scientific EffectCrosslinking:

Implementation Method 5

the purpose of crosslinking polymer chains is to connect together several polymer chains

Methodology Applied
Scientific EffectChemical bonding: Chemical Bonding

Data Source

PatentUS20240091150A1Pharmaceutical composition comprising, as thickening agent, a composition having polar media thickening properties
Publication Date: 2024.03.21 SOC DEXPLOITATION DE PROD POUR LES IND CHEM SEPPIC
  • US20240091150A1 patent drawing
  • US20240091150A1 patent drawing
  • US20240091150A1 patent drawing

AI summary

A pharmaceutical composition (F) comprising at least one pharmaceutical active principle and as thickener a composition (CA) in the form of an emulsion of the self-invertible water-in-oil type comprising, per 100% of its mass, a mass content of greater than or equal to 20% of a polymer (P) consisting of monomer units derived from partially or totally salified glutamic acid (GA), and of units derived from at least one crosslinking agent (XLA) bearing at least two glycidyl functions.