Porous Cellulose Aggregate for Tablet Disintegration

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Solution Overview

Problem

Conventional cellulose particles in pharmaceuticals and foods face challenges in achieving a balance between compactibility, fluidity, and disintegration properties, often resulting in inadequate tablet formation, poor active ingredient release, and increased production costs due to the need for complex processes and additives.

Innovation Solution

A porous cellulose aggregate with a specific secondary aggregate structure, pore volume, and particle size distribution is created, allowing for enhanced compactibility, fluidity, and disintegration properties through controlled particle entanglement and drying processes, eliminating the need for multiple processing steps and additives.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If porous cellulose particles are created using conventional methods (mixing with third component, granulating, drying, extracting), then fluidity is improved, but disintegration property deteriorates due to tight continuous cellulose wall structure

Engineering Contradiction:
ImprovefluidityVSAvoiddisintegration property
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The invention segments the cellulose structure into discrete primary particles (1-10 μm) that aggregate into porous secondary structures, rather than forming continuous film-like walls. This segmentation allows water penetration while maintaining particle integrity, resolving the contradiction between fluidity and disintegration.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates porous cellulose particles with controlled pore structures formed by aggregation of primary particles, rather than using tight continuous walls. The porous structure enables both good fluidity through particle separation and effective disintegration through water penetration into pores.

Inventive Principle:
Principle #31Porous materials

2Ease of operation

If tight continuous cellulose wall structure is formed, then fluidity is improved, but compactibility deteriorates due to poor plastic deformation

Engineering Contradiction:
ImprovefluidityVSAvoidcompactibility
Core Design Contradiction:
Ease of operationVSEase of manufacture

Solution Approach 1:

By segmenting cellulose into discrete primary particles that form aggregated secondary structures, the invention creates particles with both fluidity and plastic deformability. The segmented structure allows particles to deform under compression while maintaining cohesive integrity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite structure where primary cellulose particles aggregate into secondary porous particles, combining the advantages of individual particle fluidity with collective structural integrity for improved compactibility.

Inventive Principle:
Principle #40Composite materials

3Shape

If organic solvent and third component are used in production process, then porous structure is achieved, but production cost increases and active ingredient stability deteriorates

Engineering Contradiction:
Improveporous structureVSAvoidproduction cost
Core Design Contradiction:
ShapeVSDevice complexity

Solution Approach 1:

The invention extracts and eliminates the need for organic solvents and third components from the production process, achieving porous structure through alternative methods (spray drying of aqueous suspensions) that are simpler and more cost-effective.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention replaces expensive organic solvents and third components with simple aqueous systems that can be easily evaporated, using inexpensive, readily available materials for creating the porous structure.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

4Reliability

If pore volume within particle is increased, then disintegration property is improved, but compactibility deteriorates

Engineering Contradiction:
Improvedisintegration propertyVSAvoidcompactibility
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The invention segments the porous structure into aggregated primary particles, where the porous nature is created by inter-particle spaces rather than intra-particle voids. This allows high disintegration through water penetration into inter-particle spaces while maintaining compactibility through particle aggregation.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention shifts the pore structure from intra-particle voids to inter-particle spaces, changing the dimensional arrangement of porosity. This allows disintegration through water penetration between particles while maintaining particle integrity for good compactibility.

Inventive Principle:
Principle #17Another dimension (Dimensionality change)

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 porous cellulose aggregate improves the uniformity and bioavailability of active ingredients, reduces production costs, and enhances the stability and commercial value of formulations by ensuring efficient active ingredient release and tablet formation.

Implementation Method 1

a porous cellulose aggregate having a secondary aggregate structure formed by aggregation of primary cellulose particles, a pore volume within a particle of 0.265 cm 3

Methodology Applied
Scientific EffectCapillary action: Capillary Action

Data Source

PatentEP1873196B1Porous cellulose aggregate and molding composition thereof
Publication Date: 2016.04.13 ASAHI KASEI CHEM CORP
  • EP1873196B1 patent drawingFigure 1~2
  • EP1873196B1 patent drawingFigure 3~4
  • EP1873196B1 patent drawingFigure 5~6

AI summary

A porous cellulose aggregate characterized by having a secondary aggregate structure resulting from aggregation of primary cellulose particles, having a pore volume within a particle of 0.265 to 2.625 cm3/g, containing I-type crystals and having an average particle size of over 30 to 250 µm, a specific surface area of 0.1 to less than 20 m2/g, a repose angle of 25° to less than 44° and a swelling degree of 5% or more, and characterized by having the property of disintegrating in water.