Orally Disintegrating Tablet Bitterness Masking and Hardness

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Solution Overview

Problem

Conventional orally disintegrating tablets face challenges in achieving suitable hardness and rapid disintegrability while maintaining palatability, often requiring high compression forces that can lead to tableting failure and delayed disintegration.

Innovation Solution

The formulation includes granules A with erythritol and crystalline cellulose, and granules B with a drug and film-coating layer, combined with anhydrous calcium hydrogen phosphate and crystalline cellulose, to create an orally disintegrating tablet that can be tableted at lower compression forces, ensuring suitable hardness and rapid disintegration without bitterness.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If high compression force (15 kN or higher) is applied during tableting, then tablet hardness is improved, but disintegration time is delayed and tableting failure occurs

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

Solution Approach 1:

The invention changes the physical-chemical parameters of the formulation by incorporating specific excipients (crystalline cellulose, anhydrous calcium hydrogen phosphate, sugar alcohols) and controlling particle size parameters (700 μm or less for film-coated granules, specific size ranges for other excipients) to achieve both adequate hardness and rapid disintegration without requiring high compression forces

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses a composite formulation combining film-coated granules (700 μm or less) with specific excipients (crystalline cellulose, anhydrous calcium hydrogen phosphate, sugar alcohols, disintegrants, lubricants) in defined proportions to create a tablet that achieves both hardness and rapid disintegration through synergistic effects of multiple materials

Inventive Principle:
Principle #40Composite materials

2Strength

If high compression force is applied during tableting, then tablet hardness is improved, but tableting failure occurs

Engineering Contradiction:
Improvetablet hardnessVSAvoidtableting success rate
Core Design Contradiction:
StrengthVSReliability

Solution Approach 1:

The invention modifies formulation parameters by selecting specific excipients and their proportions, controlling particle size of film-coated granules to 700 μm or less, and optimizing the composition ratio of crystalline cellulose, anhydrous calcium hydrogen phosphate, sugar alcohols, disintegrants, and lubricants to enable tableting at reduced compression forces without failure

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention employs a composite material system where film-coated granules are combined with specific excipients in defined ratios to create a formulation that is both moldable at low compression forces and produces hard tablets, eliminating tableting failure while maintaining hardness

Inventive Principle:
Principle #40Composite materials

3Object-affected harmful factors

If film coating is applied to mask bitterness, then palatability is improved, but uniform coating requires spherical core particles of uniform particle size

Engineering Contradiction:
ImprovebitternessVSAvoidcoating uniformity requirement
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The invention controls the particle size parameter of film-coated granules to 700 μm or less and uses specific excipients with defined particle size ranges to achieve uniform coating formation, which masks bitterness while simplifying the coating process requirements

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 solution results in an orally disintegrating tablet with excellent hardness, rapid disintegration time, and improved palatability, allowing for easy administration to patients, including the elderly and those with swallowing difficulties, while maintaining effective drug elution.

Implementation Method 1

the surface of which is coated by a specific film-coating layer

Methodology Applied
Scientific EffectFilm coating: Coatings

Implementation Method 2

an orally disintegrating tablet that can be taken even without water

Methodology Applied
Scientific EffectDisintegration:

Data Source

PatentUS9744134B2Orally disintegrating tablet containing bitterness-masking granules
Publication Date: 2017.08.29 ASAHI KASEI CHEM CORP

AI summary

Disclosed is a tablet containing anhydrous calcium hydrogen phosphate, granules (A) which contain sugars, and granules (B) which contain nuclear particles having a diameter of 10-500μm, medicine and a film coating, and which have a particle diameter of 700μm or less. The present invention enables tablet-making difficulties during the manufacture of the tablet to be suppressed. In addition, the tablet has an appropriate hardness, an excellent disintegration time, and feels very good to ingest.