Orally Disintegrating Tablet With Organic Acid Coating

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Solution Overview

Problem

Intraorally disintegrating tablets face challenges in simultaneously achieving taste masking, disintegration, and controlled dissolution properties, with existing formulations often failing to maintain a stable disintegration property immediately after preparation.

Innovation Solution

Compression molding of active ingredient-containing core particles coated with a water insoluble or enteric polymer, along with an organic acid such as ascorbic acid or citric acid, to enhance taste masking and disintegration while maintaining a good dissolution profile.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If a coating layer comprising water insoluble polymer and/or enteric polymer is used, then taste masking property and dissolution property are improved, but disintegrating property immediately after preparation deteriorates

Engineering Contradiction:
Improveunpleasant taste and irritationVSAvoiddisintegrating property stability
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent applies preliminary action by incorporating a disintegrant in the coating layer before tablet formation. This pre-positioned disintegrant is prepared in advance to ensure rapid disintegration occurs immediately after tablet preparation, counteracting the potential deterioration of disintegrating properties that would otherwise result from using polymer coatings for taste masking and controlled dissolution.

Inventive Principle:
Principle #10Preliminary action

2Adaptability or versatility

If multiple properties (taste masking, disintegration, controlled dissolution) are simultaneously targeted, then formulation complexity increases, but quality stability deteriorates

Engineering Contradiction:
Improvemultiple functional propertiesVSAvoidquality formulation stability
Core Design Contradiction:
Adaptability or versatilityVSStability of the object's composition

Solution Approach 1:

The patent merges multiple functions into a single integrated coating layer that simultaneously provides taste masking (through polymer coating), disintegration (through incorporated disintegrant), and controlled dissolution (through water insoluble/enteric polymer). This consolidation of multiple functions into one coating system maintains quality formulation stability while achieving all desired properties.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The coating layer is formulated as a composite material combining water insoluble polymer, enteric polymer, and disintegrant in specific proportions. This composite structure enables the coating to simultaneously provide taste masking, rapid disintegration, and controlled dissolution properties while maintaining stable and reproducible formulation quality.

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 approach results in intraorally disintegrating tablets that effectively mask bitterness and irritation, with improved disintegration and dissolution properties, retaining performance immediately after preparation.

Implementation Method 1

an intraorally disintegrating tablet... comprising an organic acid as a disintegration accelerator

Methodology Applied
Scientific EffectpH-dependent disintegration acceleration:

Implementation Method 2

a property of masking unpleasant tastes such as bitterness derived from the active ingredient and an irritating sensation

Methodology Applied
Scientific EffectTaste masking:

Implementation Method 3

a dissolution property intended for the intestinal tract... an enteric polymer such as a methacrylic acid copolymer

Methodology Applied
Scientific EffectpH-dependent dissolution control:

Data Source

PatentEP2591774B1Orally disintegrating tablet
Publication Date: 2020.05.27 TEIJIN PHARMA CO LTD

AI summary

Disclosed is an orally disintegrating tablet which masks bitterness, dissolves well, and which permanently retains good oral disintegration properties immediately following manufacture. The disclosed orally disintegrating tablet is formed by compression-molding an organic acid together with particles comprising active ingredient-containing nuclear particles covered by a layer containing water-insoluble polymers and/or enteric polymers.