Micro-fibrillated Cellulose Disintegrating Composition for Tablets

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Solution Overview

Problem

There is a lack of effective disintegrative particulate compositions and tablets that utilize the excellent properties of micro-fibrillated cellulose for pharmaceuticals and foods, particularly for individuals with swallowing difficulties, such as the elderly and children, who require convenient and water-independent forms.

Innovation Solution

A disintegrative particulate composition comprising micro-fibrillated cellulose with an average fiber length of 0.01~2 mm and diameter of 0.001~1µm, combined with disintegrator components like crospovidone, croscarmellose sodium, and starch, which enhances tablet hardness and reduces disintegration time in water through a synergistic effect.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If conventional disintegrators are used alone, then disintegration function is achieved, but tablet hardness is insufficient

Engineering Contradiction:

Improvetablet hardnessVSAvoiddisintegration function

Core Design Contradiction:

StrengthVSReliability

Solution Approach 1:

The patent combines micro-fibrillated cellulose with conventional disintegrators (crospovidone, croscarmellose sodium, starch, etc.) to create a composite disintegrating composition. This composite material achieves both adequate tablet hardness and reliable disintegration function, resolving the contradiction between mechanical strength and disintegration performance.

Inventive Principle:

Principle #40Composite materials

2Stability of the object's composition

If micro-fibrillated cellulose is used alone, then water retention and form retention are improved, but disintegration speed is insufficient

Engineering Contradiction:

Improveform retentionVSAvoiddisintegration time

Core Design Contradiction:

Stability of the object's compositionVSLoss of time

Solution Approach 1:

By combining micro-fibrillated cellulose (which provides form retention and water resistance) with conventional disintegrators (which provide rapid disintegration), the patent creates a composite that achieves both form stability and fast disintegration, resolving the contradiction between composition stability and disintegration speed.

Inventive Principle:

Principle #40Composite materials

3Loss of time

If high amounts of disintegrator are used, then disintegration time is reduced, but tablet hardness decreases

Engineering Contradiction:

Improvedisintegration timeVSAvoidtablet hardness

Core Design Contradiction:

Loss of timeVSStrength

Solution Approach 1:

The patent optimizes the composition parameters by combining micro-fibrillated cellulose with conventional disintegrators in specific ratios. This parameter optimization allows achieving rapid disintegration (1-60 seconds) while maintaining adequate tablet hardness (20-200 N), resolving the contradiction between disintegration speed and mechanical strength.

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 composition provides tablets with excellent hardness and disintegrability, achieving disintegration times of 1-60 seconds and hardness of 20-200 N, making them suitable for pharmaceuticals and food applications.

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 EffectHydrogen bonding:

Implementation Method 3

tablet hardness of the various kinds of disintegrating tablets comprising said composition shall be increased while disintegration time in water shall be shortened due to a synergistic effect

Methodology Applied

Scientific EffectSynergistic effect:

Implementation Method 4

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

Methodology Applied

Scientific EffectHydrophilic property: Hydrophile

Data Source

PatentEP3135300B1Disintegrating particle composition including microfibrous cellulose

Publication Date: 2022.03.30 DAICEL CORP

AI summary

The purpose of the present invention is to provide a disintegrating tablet having excellent tablet hardness and disintegrability, which is suitable for pharmaceuticals and various kinds of foods such as supplemental foods, nutrition function foods and health foods has been desired as highly convenient forms which can safely be taken by patients who have difficulty in swallowing drugs, elderly people, children, etc., and which can easily be taken without water irrespective of places; and a disintegrative particulate composition comprised in the disintegrating tablet. The present invention relates to a disintegrative particulate composition comprising a disintegrator component and micro-fibrillated cellulose, and a disintegrating tablet for pharmaceuticals or foods, comprising the disintegrative particulate composition, which has excellent tablet hardness and disintegrability.