Spray Drying Polymer Dispersion for Pharmaceutical Coating

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Solution Overview

Problem

Current pharmaceutical coating technologies face challenges in producing free-flowing powdery film coating agents with good redispersibility that maintain release behavior stability under prolonged or temperature-stressed storage, and they often result in undesirable agglomeration and high mechanical strength issues.

Innovation Solution

A process involving radical emulsion polymerization of N,N-diethylaminoethyl methacrylate and esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids, followed by spray drying with controlled inlet and outlet temperatures to produce powders with specific glass transition and film-forming temperatures, ensuring the powders are free-flowing and redispersible without agglomeration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If spray drying is used to convert aqueous polymer dispersion into powder, then free-flowing powder with good redispersibility is obtained, but agglomeration occurs and mechanical strength increases undesirably

Engineering Contradiction:
ImproveredispersibilityVSAvoidmechanical strength
Core Design Contradiction:
Ease of operationVSStrength

Solution Approach 1:

The patent applies parameter changes by carefully controlling the glass transition temperature (Tg) of the polymer to be between 40-80°C and the minimum film-forming temperature (MFFT) to be between 30-70°C. These specific temperature parameters prevent agglomeration during storage while maintaining low mechanical strength, resolving the contradiction between redispersibility and mechanical strength.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses composite materials by combining N,N-diethylaminoethyl methacrylate with specific esters of α,β-ethylenically unsaturated mono- and dicarboxylic acids. This composite polymer structure achieves the desired balance of redispersibility and low mechanical strength by incorporating both functional components in specific ratios.

Inventive Principle:
Principle #40Composite materials

2Reliability

If prolonged or temperature-stressed storage is applied to coating agents, then stability of release behavior is tested, but agglomeration occurs and redispersibility deteriorates

Engineering Contradiction:
Improvestability of release behaviorVSAvoidredispersibility
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent applies beforehand cushioning by pre-setting the glass transition temperature and minimum film-forming temperature within specific ranges before storage. This preventive measure ensures that even under prolonged or temperature-stressed storage conditions, the powder maintains its redispersibility and release behavior stability without agglomeration.

Inventive Principle:
Principle #11Beforehand cushioning (Prior cushioning)

3Strength

If high mechanical strength is achieved in powder coating, then coating durability improves, but unpleasant mouthfeel occurs due to coarse-grained disintegrants

Engineering Contradiction:
Improvemechanical strengthVSAvoidmouthfeel
Core Design Contradiction:
StrengthVSObject-affected harmful factors

Solution Approach 1:

The patent changes the mechanical strength parameter by controlling the polymer's glass transition temperature and minimum film-forming temperature to specific ranges, resulting in low mechanical strength that prevents coarse-grained disintegration. This eliminates the unpleasant mouthfeel while maintaining sufficient coating durability through the controlled polymer composition.

Inventive Principle:
Principle #35Parameter changes

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 powders are highly redispersible, maintain release behavior stability, and exhibit low mechanical strength, preventing unpleasant mouthfeel and ensuring rapid release in acidic environments while protecting moisture-sensitive active ingredients.

Implementation Method 1

spray-drying a polymer dispersion to produce coating solutions

Methodology Applied
Scientific EffectEvaporation: Evaporation

Implementation Method 2

the inlet temperature of the drying gas is at least 20 °C above the glass transition temperature and at least 20 °C above the minimum film forming temperature

Methodology Applied
Scientific EffectHeat transfer: Conduction (thermal)

Implementation Method 3

radical emulsion polymerization of a monomer mixture containing N,N-diethylaminoethyl methacrylate

Methodology Applied
Scientific EffectRadical polymerization: Photopolymerisation

Implementation Method 4

the inlet temperature of the drying gas is at least 20 °C above the glass transition temperature

Methodology Applied
Scientific EffectGlass transition:

Implementation Method 5

converted an aqueous dispersion into a free-flowing powder with good redispersibility using a spray process

Methodology Applied
Scientific EffectAtomization: Fluid Spray

Data Source

PatentEP2681264B1Process for making powder coating compositions for stable protecting coating for pharmaceutical dosage forms
Publication Date: 2017.08.02 BASF SE

AI summary

The invention relates to a method for producing powdery coating agents from aqueous polymer dispersions, containing i) as component A a polymer, obtained by radical polymerization, made of a) N,N-diethylaminoethyl methacrylate, and b) at least one radically polymerizable compound, selected among esters of a,ß-ethylenically unsaturated monocarboxylic and dicarboxylic acids containing C1-C8-alkanols, characterized in that the aqueous polymer dispersion is transferred into a powder by spray methods in the presence of a drying gas, wherein the input temperature of the drying gas in the spray device is at least 20ºC above the glass transition temperature and at least 20ºC above the minimum film formation temperature of the polymer, and the output temperature of the drying gas from the spray device is maintained at 40 to 85ºC.