Fine-Particle Crosslinked PVP Tablet Disintegrant

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Solution Overview

Problem

Coarse crosslinked polyvinylpyrrolidone disintegrants in tablets lead to a rough surface, low resistance to crushing, inhomogeneous mixing, segregation, and an unpleasant mouthfeel, while smaller particle sizes result in reduced disintegrant effect and increased moisture sensitivity.

Innovation Solution

Fine-particle crosslinked polyvinylpyrrolidone with an average particle size of 5-60 μm and hydration capacity greater than 7 g/g, prepared through popcorn polymerization, which can be controlled by inert gas flow and polymerization conditions, is used as a tablet disintegrant.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If coarse crosslinked polyvinylpyrrolidone (particle size >100 μm) is used as tablet disintegrant, then good disintegrant effect is achieved, but tablet surface becomes rough, resistance to crushing decreases, mixing becomes inhomogeneous, and segregation occurs

Engineering Contradiction:
Improvedisintegrant effectVSAvoidtablet surface smoothness
Core Design Contradiction:
Duration of action of moving objectVSManufacturing precision

Solution Approach 1:

The patent changes the critical parameter of particle size from coarse (>100 μm) to fine (5-60 μm) while maintaining the crosslinked polyvinylpyrrolidone chemistry. This parameter change resolves the contradiction by providing both smooth tablet surfaces and adequate disintegrant effect, as the fine particles eliminate surface roughness and segregation while the crosslinked structure maintains disintegration capability.

Inventive Principle:
Principle #35Parameter changes

2Manufacturing precision

If fine crosslinked polyvinylpyrrolidone (particle size 5-60 μm) is used as tablet disintegrant, then smooth tablet surface and homogeneous mixing are achieved, but disintegrant effect is reduced and moisture sensitivity increases

Engineering Contradiction:
Improvetablet surface smoothnessVSAvoiddisintegrant effect
Core Design Contradiction:
Manufacturing precisionVSDuration of action of moving object

Solution Approach 1:

The patent creates a composite material system combining fine particle size (5-60 μm) with crosslinked polyvinylpyrrolidone chemistry. This composite approach allows the fine particles to provide smooth surfaces and homogeneous mixing while the crosslinked structure maintains high disintegrant effect and reduces moisture sensitivity, resolving the contradiction between fine particle benefits and disintegrant performance.

Inventive Principle:
Principle #40Composite materials

3Duration of action of moving object

If higher concentration of small-particle disintegrant is used to achieve adequate disintegrant effect, then disintegration is improved, but costs increase and tablets become more moisture-sensitive

Engineering Contradiction:
Improvedisintegrant effectVSAvoidmoisture sensitivity
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent changes the particle size parameter to fine (5-60 μm) which increases the surface area to volume ratio, thereby enhancing the disintegrant effect per unit mass. This allows achievement of adequate disintegrant effect at lower concentrations, reducing both costs and moisture sensitivity issues associated with higher concentrations of coarse particles.

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 fine-particle disintegrants provide a smooth tablet surface, high resistance to crushing, homogeneous mixing, and a pleasant mouthfeel, maintaining disintegrant effect even under moist conditions, suitable for fast-disintegrating tablets and wet granulation processes.

Implementation Method 1

crosslinked polyvinylpyrrolidone with an average particle size of from 5 to 60 μm and a hydration capacity greater than 7 g/g

Methodology Applied
Scientific EffectHydration: Hydrates

Data Source

PatentUS8597679B2Fine-particle crosslinked polyvinylpyrrolidone as tablet disintegrant
Publication Date: 2013.12.03 BASF SE
  • US8597679B2 patent drawing

AI summary

Use of crosslinked polyvinylpyrrolidone with an average particle size of 5-60 μm and a hydration capacity of greater than 7 g/g as tablet disintegrant.