Aqueous Polymer Dispersion for pH-Dependent Solubility

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Solution Overview

Problem

Existing processes for preparing pharmaceutical coatings lack ease of preparation and often require elaborate drying or finishing steps, and existing polymers do not adequately provide pH-dependent solubility, water vapor barrier properties, or effective taste masking for active ingredients.

Innovation Solution

Aqueous polymer dispersions are prepared by free-radical emulsion polymerization of a monomer mixture comprising N,N-diethylaminoethyl methacrylate and esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids in an aqueous medium at a pH of at least 8, allowing for the formation of polymer films with pH-dependent solubility and improved barrier properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If solution polymerization in organic solvent is used, then polymer coatings can be prepared, but the preparation process becomes complex and requires elaborate drying or finishing steps

Engineering Contradiction:
Improveease of preparationVSAvoidprocess complexity
Core Design Contradiction:
Ease of manufactureVSDevice complexity

Solution Approach 1:

The invention changes the polymerization medium from organic solvent to aqueous medium, and maintains polymerization at pH ≥ 8 throughout the process. This parameter change eliminates the need for elaborate drying or finishing steps while simplifying the overall preparation process, directly resolving the contradiction between ease of manufacture and process complexity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses aqueous polymer dispersions as a substitute for traditional organic solvent-based polymer coatings. The aqueous dispersion can be directly applied and forms functional coatings without requiring the complex drying and finishing steps needed for organic solvent systems, thereby simplifying the manufacturing process

Inventive Principle:
Principle #26Copying

2Adaptability or versatility

If copolymers based on N,N-dialkylaminoalkyl(meth)acrylates are used, then pH-dependent solubility is achieved, but the ester group is prone to hydrolysis in basic medium

Engineering Contradiction:
ImprovepH-dependent solubilityVSAvoidchemical stability
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The invention uses composite copolymer structures combining N,N-diethylaminoethyl methacrylate with hydrophobic monomers (esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids). This composite approach provides both pH-dependent solubility through the amino group and enhanced chemical stability by incorporating hydrolysis-resistant ester groups, resolving the contradiction between adaptability and reliability

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The invention localizes the pH-responsive functionality specifically to the N,N-diethylaminoethyl methacrylate units while the hydrophobic comonomer units provide structural stability and resistance to hydrolysis. This local quality differentiation allows the polymer to exhibit pH-dependent solubility without sacrificing chemical stability in basic medium

Inventive Principle:
Principle #3Local quality

3Adaptability or versatility

If polymer films with pH-dependent solubility are used, then taste masking and controlled release are improved, but water vapor barrier properties are insufficient

Engineering Contradiction:
ImprovepH-dependent solubilityVSAvoidwater vapor permeability
Core Design Contradiction:
Adaptability or versatilityVSObject-affected harmful factors

Solution Approach 1:

The invention creates composite copolymer films combining N,N-diethylaminoethyl methacrylate units (providing pH-dependent solubility for taste masking and controlled release) with hydrophobic ester comonomer units (providing water vapor barrier properties). This composite structure simultaneously achieves pH-responsive functionality and effective water vapor protection, resolving the contradiction between adaptability and harmful factor resistance

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The invention assigns different local functions to different polymer units: the N,N-diethylaminoethyl methacrylate units provide pH-dependent solubility for taste masking and controlled release, while the hydrophobic comonomer units locally provide water vapor barrier properties. This functional differentiation within the polymer structure resolves the contradiction between pH-responsive adaptability and water vapor protection

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 resulting polymer films exhibit excellent pH-dependent solubility, water vapor barrier properties, and effective taste masking, enabling stable and rapid release of active ingredients while maintaining stability and flexibility, even in acidic environments.

Implementation Method 1

free-radical emulsion polymerization of a monomer mixture which comprises N,N-diethylaminoethyl methacrylate

Methodology Applied
Scientific EffectFree-radical polymerization: Photopolymerisation

Implementation Method 2

applied in the form of a film, for example by casting, spreading or spraying, and subsequent drying or gelation

Methodology Applied
Scientific EffectEvaporation: Evaporation

Data Source

PatentUS9732200B2Aqueous polymer dispersion based on N,N-diethylaminoethyl methacrylate, its preparation and use
Publication Date: 2017.08.15 BASF SE
  • US9732200B2 patent drawing

AI summary

The present invention relates to a process for preparing an aqueous polymer dispersion by free-radical emulsion polymerization of a monomer mixture which comprises N,N-diethylaminoethyl methacrylate, to the polymer dispersion obtainable by this process, and to the use thereof.