Orally Disintegrating Tablet Hardness and Disintegration

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Solution Overview

Problem

Existing orally disintegrating tablets face challenges in achieving quick disintegration, favorable taste, sufficient hardness, and storage stability while being easy to produce industrially without requiring special equipment.

Innovation Solution

Incorporating crystalline cellulose with a bulk density of 0.23 g/cm³ or less, a sugar alcohol, and pregelatinized starch, along with optional disintegrating and lubricating agents, to create a tablet that can be produced by conventional compression, ensuring quick disintegration and solubility in the oral cavity and maintaining hardness during production and storage.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If conventional tablets are made with sufficient hardness for production and transportation, then they can tolerate physical impacts, but they disintegrate slowly in the oral cavity

Engineering Contradiction:
Improvetablet hardnessVSAvoiddisintegration speed
Core Design Contradiction:
StrengthVSSpeed

Solution Approach 1:

The patent uses a composite formulation combining mannitol (sugar alcohol) as the main excipient with specific disintegrating agents (crosslinked polyvinyl polymer, carboxymethyl cellulose calcium salt, or sodium starch glycolate) in controlled amounts. This composite structure allows the tablet to maintain hardness from mannitol's crystalline structure while the disintegrating agents create rapid water absorption and swelling, enabling simultaneous achievement of sufficient hardness and quick disintegration within 5-120 seconds.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent optimizes the content ratios of specific components: mannitol (5-95 wt%), disintegrating agents (1-30 wt% each), and optional excipients (1-20 wt%). By precisely controlling these parameters, particularly the disintegrating agent content within specific ranges, the tablet achieves the desired balance between mechanical strength for handling and rapid disintegration in oral cavity.

Inventive Principle:
Principle #35Parameter changes

2Speed

If disintegrating agents are added to achieve quick oral disintegration, then the tablet disintegrates rapidly, but the tablet hardness decreases

Engineering Contradiction:
Improvedisintegration speedVSAvoidtablet hardness
Core Design Contradiction:
SpeedVSStrength

Solution Approach 1:

The patent specifies optimal content ranges for disintegrating agents (crosslinked polyvinyl polymer, carboxymethyl cellulose calcium salt, or sodium starch glycolate) at 1-30 wt% each, with total disintegrating agent content controlled at 5-60 wt% of the tablet. This precise parameter control ensures sufficient disintegration speed while maintaining adequate hardness through the dominant mannitol matrix.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The composite formulation uses mannitol as the structural backbone providing hardness, while incorporating controlled amounts of disintegrating agents that provide rapid water absorption and swelling. The synergistic combination allows both properties to coexist: mannitol's crystalline structure maintains mechanical integrity during handling, while the disintegrating agents enable rapid disintegration in oral cavity within 5-120 seconds.

Inventive Principle:
Principle #40Composite materials

3Reliability

If bitter-tasting drugs are used, then the therapeutic effect is achieved, but the taste is unpleasant and causes irritation

Engineering Contradiction:
Improvetherapeutic effectVSAvoidunpleasant taste and irritation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses mannitol (sugar alcohol) as a taste-masking intermediary that provides a pleasant sweet taste and masks the bitter taste of drugs. The mannitol serves as both the main excipient and a taste-modifying agent, creating a favorable overall taste perception while the drug maintains its therapeutic effect. This intermediary approach allows co-administration of bitter drugs with pleasant taste characteristics.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Ease of operation

If the tablet is made to disintegrate quickly in the mouth, then ease of intake is improved, but the tablet lacks sufficient hardness for production and transportation

Engineering Contradiction:
Improveease of intakeVSAvoidtablet hardness
Core Design Contradiction:
Ease of operationVSStrength

Solution Approach 1:

The patent employs a composite formulation where mannitol (5-95 wt%) provides the structural framework and mechanical strength necessary for production and transportation, while specific disintegrating agents (crosslinked polyvinyl polymer, carboxymethyl cellulose calcium salt, or sodium starch glycolate at 1-30 wt% each) provide rapid water absorption and swelling capabilities. This composite structure enables the tablet to maintain sufficient hardness for handling while achieving quick disintegration within 5-120 seconds in the oral cavity, thus improving ease of intake for elderly, children, and aphagia patients.

Inventive Principle:
Principle #40Composite materials

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 resulting tablets disintegrate within 5 to 120 seconds, provide favorable taste, and exhibit excellent storage stability, making them suitable for elderly and pediatric use, while being easily producible without complex equipment or processes.

Implementation Method 1

incorporating a crystalline cellulose having a bulk density of 0.23 g/cm³ or less

Methodology Applied
Scientific EffectBulk density:

Implementation Method 2

incorporating a crystalline cellulose having a bulk density of 0.23 g/cm³ or less, a sugar alcohol, and pregelatinized starch

Methodology Applied
Scientific EffectAbsorption: Absorption (physical)

Implementation Method 3

incorporating a crystalline cellulose having a bulk density of 0.23 g/cm³ or less, a sugar alcohol, and pregelatinized starch, along with optional disintegrating and lubricating agents, to create a tablet that can be produced by conventional compression

Methodology Applied
Scientific EffectCompression: Compression

Data Source

PatentEP2842549B1Orally disintegrating tablet and method for producing same
Publication Date: 2018.08.08 DAIICHI SANKYO CO LTD

AI summary

Provided are an orally disintegrating tablet that quickly disintegrates when it is placed in the mouth or put into water, provides favorable taste, has a sufficient hardness in general production, transportation and use and is excellent in terms of storage stability, and a process for the production of the same which is excellent in terms of industrial production. An orally disintegrating tablet containing a drug, a crystalline cellulose having a bulk density of 0.23 g/cm3 or less (preferably from 0.10 g/cm3 to 0.23 g/cm3), a sugar alcohol and a pregelatinized starch.