Micro-fibrillated Cellulose Disintegrator for High-Concentration Tablets

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Solution Overview

Problem

Existing disintegrating tablets do not effectively incorporate high concentrations of active ingredients such as medicinal, nutritional, and food components, and lack efficient disintegration properties.

Innovation Solution

A composition comprising micro-fibrillated cellulose as the sole disintegrator component, with an active ingredient concentration of 80-90 wt%, achieving excellent tablet hardness and disintegrability without additional disintegrators.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If multiple disintegrators are used in addition to micro-fibrillated cellulose, then tablet hardness increases due to synergistic effect, but disintegration time in water becomes shorter and formulation complexity increases

Engineering Contradiction:
Improvetablet hardnessVSAvoidformulation complexity
Core Design Contradiction:
StrengthVSDevice complexity

Solution Approach 1:

The invention extracts and isolates the disintegrator function to micro-fibrillated cellulose alone, removing other disintegrators from the formulation. This simplification maintains tablet hardness through optimized micro-fibrillated cellulose content (1-20 wt%) while achieving rapid disintegration, thereby resolving the contradiction between formulation complexity and performance.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention changes the parameter of disintegrator composition from multiple components to a single component (micro-fibrillated cellulose), and optimizes its concentration parameter (1-20 wt%) to achieve both adequate tablet hardness and rapid disintegration, eliminating the need for synergistic combinations of multiple disintegrators.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If micro-fibrillated cellulose is used as the sole disintegrator, then active ingredient concentration can be increased to 80-90 wt%, but tablet formulation requires precise optimization

Engineering Contradiction:
Improveactive ingredient concentrationVSAvoidformulation optimization precision
Core Design Contradiction:
Quantity of substanceVSManufacturing precision

Solution Approach 1:

The invention changes the formulation parameter by using micro-fibrillated cellulose at optimized concentrations (1-20 wt%) as the sole disintegrator, enabling active ingredient concentration to reach 80-90 wt%. The specific parameter optimization provides a clear numerical range that balances high active ingredient content with adequate tablet hardness and disintegration performance.

Inventive Principle:
Principle #35Parameter changes

3Device complexity

If conventional cellulose is used as disintegrator, then formulation is simple, but disintegration performance and water-retaining property are insufficient

Engineering Contradiction:
Improveformulation simplicityVSAvoiddisintegration performance
Core Design Contradiction:
Device complexityVSReliability

Solution Approach 1:

The invention changes the physical parameter of cellulose from conventional forms to micro-fibrillated form with fiber diameter of a few nm to a few μm. This parameter change dramatically improves surface area, hydrophilic property, and three-dimensional network formation, achieving excellent disintegration performance and water-retaining properties while maintaining formulation simplicity through single-component use.

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 use of micro-fibrillated cellulose allows for high active ingredient concentration and rapid disintegration in water, with tablet hardness ranging from 10 to 200 N and disintegration time of 6 minutes or less, enhancing the production and performance of disintegrating tablets.

Implementation Method 1

a surface area has been increased, hydrophilic property that is the original characteristics of cellulose has been significantly strengthened, and a three-dimensional network has been formed

Methodology Applied
Scientific EffectCapillary action: Capillary Action

Implementation Method 2

hydrophilic property that is the original characteristics of cellulose has been significantly strengthened

Methodology Applied
Scientific EffectHydrophilic interaction: Hydrophile

Implementation Method 3

a three-dimensional network has been formed, without deteriorating basic properties such as physical and chemical stabilities

Methodology Applied
Scientific EffectHydrogen bonding: Chemical Bonding

Data Source

PatentEP3626272B1Composition for disintegrating tablets containing microfibrous cellulose and active ingredient
Publication Date: 2023.10.04 DAICEL CORP

AI summary

The purpose of the present invention is to provide various kinds of disintegrating tablets having various purposes and applications, such as for pharmaceuticals Chinese medicine and various kinds of foods and comprising various kinds of active ingredients such as the medicinal or nutritional ingredient, the supplement and the food component at a high concentration; and a composition for the disintegrating tablets. The present invention relates to a composition for a disintegrating tablet, comprising a disintegrator component consisting of only micro-fibrillated cellulose, and an active ingredient; and a disintegrating tablet for pharmaceuticals or foods, comprising the composition.