Antioxidant-Integrated Polymer Powder for Pharmaceutical Coatings

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Solution Overview

Problem

There is a need for free-flowing pulverulent film coating compositions with good redispersibility in water that maintain stability during prolonged or thermally demanding storage, without changes in release behavior or discoloration, and that can incorporate sparingly water-soluble antioxidants effectively into pharmaceutical dosage forms.

Innovation Solution

A process involving the radical polymerization of N,N-diethylaminoethyl methacrylate and esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids, where antioxidants are incorporated into an aqueous polymer dispersion and converted to powder form through spray processing with controlled drying gas temperatures, ensuring the antioxidants are evenly distributed and the polymer maintains stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If antioxidants are incorporated into aqueous polymer dispersion, then stability during storage is improved, but water solubility of antioxidants is limited

Engineering Contradiction:
Improvestability during storageVSAvoidwater solubility of antioxidants
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent uses an emulsifier as an intermediary substance to incorporate sparingly water-soluble antioxidants into the aqueous polymer dispersion. The emulsifier acts as a mediator that enables the antioxidant to disperse uniformly in the water-based system despite its limited water solubility, thereby achieving stability during storage without requiring high water solubility of the antioxidant itself.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If spray drying is used to convert dispersion to powder, then redispersibility is improved, but particle size control becomes critical

Engineering Contradiction:
ImproveredispersibilityVSAvoidparticle size control
Core Design Contradiction:
Ease of operationVSManufacturing precision

Solution Approach 1:

The patent controls the particle size and redispersibility by optimizing spray drying parameters including inlet temperature (80-150°C), outlet temperature (40-80°C), and atomization pressure (1-5 bar). By adjusting these parameters, the process achieves optimal particle size distribution that ensures good redispersibility while maintaining manufacturing control.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If high drying gas temperature is used, then drying efficiency is improved, but polymer stability may deteriorate

Engineering Contradiction:
Improvedrying efficiencyVSAvoidpolymer stability
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent employs dynamic temperature control in the spray drying process, using high inlet temperatures (80-150°C) for efficient drying while maintaining outlet temperatures (40-80°C) that protect polymer stability. The system dynamically balances drying efficiency and polymer stability through controlled temperature gradients and residence time management.

Inventive Principle:
Principle #15Dynamics

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 powders exhibit excellent redispersibility, stability, and controlled release properties, with antioxidants effectively integrated into the polymer particles, preventing agglomeration and maintaining performance under stress conditions.

Implementation Method 1

the aqueous dispersion is converted to powder form by spraying processes

Methodology Applied
Scientific EffectEvaporation: Evaporation

Implementation Method 2

A process for producing pulverulent, antioxidant-comprising coating compositions of aqueous polymer dispersions comprising, as component A, a polymer obtained by radical polymerization of

Methodology Applied
Scientific EffectRadical polymerization: Photopolymerisation

Data Source

PatentUS8962064B2Production of pulverulent coating compositions for stable protective coatings for pharmaceutical dosage forms
Publication Date: 2015.02.24 BASF SE

AI summary

Described is a process for producing pulverulent, antioxidant-comprising coating compositions, comprising providing an aqueous polymer dispersions comprising one or more antioxidants and a polymer obtained by radical polymerization ofa) N,N-diethylaminoethyl methacrylate, andb) at least one radically polymerizable compound selected from esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids with C1-C8-alkanols,wherein the antioxidants are incorporated into the aqueous polymer dispersion in the form of a solution or of a dispersion, and spray processing the aqueous polymer dispersion to provide a powder form.