Orally Disintegrating Tablet Hardness and Disintegration Trade-off

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Solution Overview

Problem

Conventional ultrafast-disintegrating tablets have low tablet hardness and require specialized freeze-drying equipment, limiting production efficiency and practical application.

Innovation Solution

Development of an orally disintegrating tablet with a specific surface area of 1.60 to 2.30 mm²/mg, weight of 10 to 50 mg, and tablet hardness of 10 to 21 N, using a disintegrative particulate composition comprising acid-type carboxymethylcellulose, other disintegrators, and excipients, produced through a conventional tableting process without freeze-drying.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If molding pressure is increased to increase tablet hardness, then tablet hardness is improved, but disintegration time is prolonged

Engineering Contradiction:
Improvetablet hardnessVSAvoiddisintegration time
Core Design Contradiction:
StrengthVSDuration of action of moving object

Solution Approach 1:

The patent changes the physical and chemical parameters of the tablet formulation by incorporating specific disintegrants (crospovidone, sodium starch glycolate, cross-linked carboxymethyl cellulose) in optimized proportions. These disintegrants have specific swelling ratios and disintegration characteristics that allow the tablet to disintegrate rapidly even under high compression forces, thus resolving the contradiction between hardness and disintegration time

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses a composite formulation combining multiple disintegrants with different mechanisms of action (superdisintegrants that swell, those that form channels, and those that weaken bonds). This composite approach creates a synergistic effect where the tablet maintains structural integrity for handling while containing multiple pathways for rapid disintegration upon contact with moisture

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If molding pressure is reduced to shorten disintegration time, then disintegration time is shortened, but tablet hardness is reduced

Engineering Contradiction:
Improvedisintegration timeVSAvoidtablet hardness
Core Design Contradiction:
Duration of action of moving objectVSStrength

Solution Approach 1:

The patent modifies the formulation parameters by selecting disintegrants with high swelling ratios and rapid water absorption characteristics. These disintegrants are present in sufficient quantities to ensure rapid disintegration even when compression force is reduced, allowing the tablet to break down quickly without requiring high molding pressure to maintain hardness

Inventive Principle:
Principle #35Parameter changes

3Duration of action of moving object

If freeze-drying is used to achieve ultrafast disintegration, then disintegration time is shortened, but production complexity and cost are increased

Engineering Contradiction:
Improvedisintegration timeVSAvoidproduction process complexity
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent extracts and eliminates the freeze-drying step from the production process, replacing it with conventional tableting equipment. The disintegration function previously achieved through freeze-dried porous structures is now achieved through chemically active disintegrants incorporated into the tablet matrix, simplifying the manufacturing process while maintaining ultrafast disintegration performance

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent replaces expensive, complex freeze-drying equipment and processes with inexpensive, conventional tableting machinery. The disintegration function is achieved through affordable disintegrant ingredients rather than costly processing equipment, making ultrafast-disintegrating tablets economically viable for mass production

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

Data Source

PatentEP3238712B1Very rapidly disintegrating tablet, and method for producing same
Publication Date: 2023.11.01 DAICEL CORP
  • EP3238712B1 patent drawingFigure 1

AI summary

An object of the present invention is to provide an orally disintegrating tablet (ultrafast-disintegrating tablet) having an extremely high disintegrability (short disintegration time), and a high tablet hardness, and to provide a simple method for the production of said ultrafast-disintegrating tablet without such a complicated process as freeze-drying. This invention relates to an orally disintegrating tablet having a specific surface area of from 1.50 to 2.50 mm2/mg and a weight of from 10 to 50 mg, particularly having a disintegration time in water of 7 seconds or less and an oral disintegration time of 5 seconds or less, a method for the production of said orally disintegrating tablet, and to a disintegrative particulate composition for use in said method.