Orally Disintegrating Tablet Additive Composition for Hardness and Disintegration

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Solution Overview

Problem

Existing orally disintegrating tablets face challenges in achieving quick disintegrability and maintaining hardness, with existing formulations either taking too long to disintegrate or becoming too soft when stored under humid conditions.

Innovation Solution

A novel additive composition for orally disintegrating tablets, comprising D-mannitol, low-substituted hydroxypropyl cellulose, and microcrystalline cellulose, with crospovidone, in a specific ratio, and a producing method using fluidized bed granulation with water as the granulation liquid, to achieve the desired disintegration time and hardness.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Loss of time

If conventional additives are used to achieve quick disintegrability, then disintegration time is reduced, but tablet hardness becomes insufficient

Engineering Contradiction:

Improvedisintegration timeVSAvoidtablet hardness

Core Design Contradiction:

Loss of timeVSStrength

Solution Approach 1:

The patent uses a composite additive system comprising low-substituted hydroxypropyl cellulose (L-HPC) combined with crospovidone and microcrystalline cellulose in specific ratios. This composite approach allows L-HPC to provide quick disintegration while crospovidone and microcrystalline cellulose contribute to tablet hardness, resolving the contradiction between fast disintegration and adequate hardness that plagues conventional single-additive formulations.

Inventive Principle:

Principle #40Composite materials

2Strength

If additives are increased to maintain tablet hardness, then hardness is improved, but disintegration time increases

Engineering Contradiction:

Improvetablet hardnessVSAvoiddisintegration time

Core Design Contradiction:

StrengthVSLoss of time

Solution Approach 1:

The patent optimizes the ratio parameters of the additive components, specifically setting L-HPC at 90-99.9 mass%, crospovidone at 0.1-10 mass%, and microcrystalline cellulose at 0.1-10 mass%. By precisely controlling these compositional parameters, the formulation achieves the optimal balance where sufficient hardness is maintained while disintegration time remains within 30 seconds, reversing the traditional trade-off.

Inventive Principle:

Principle #35Parameter changes

3Loss of time

If conventional formulations are used to achieve quick disintegration, then disintegration speed is improved, but humidity resistance deteriorates

Engineering Contradiction:

Improvedisintegration timeVSAvoidhumidity resistance

Core Design Contradiction:

Loss of timeVSReliability

Solution Approach 1:

The patent employs a composite material system where L-HPC serves as the primary disintegrant providing quick disintegration, while microcrystalline cellulose acts as a humidity-resistant filler that maintains tablet structural integrity. This composite approach allows the tablet to disintegrate quickly in the oral cavity while resisting humidity-induced degradation during storage, resolving the contradiction between disintegration speed and humidity resistance.

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 additive composition ensures orally disintegrating tablets disintegrate within 30 seconds or less with saliva or water, maintains hardness across varying tableting pressures, and exhibits improved humidity resistance, preventing significant thickness increase and hardness loss during storage.

Implementation Method 1

low-substituted hydroxypropyl cellulose and crospovidone, in a ratio of 5:4, wherein the low-substituted hydroxypropyl cellulose and the crospovidone provide a quick disintegrability to the orally disintegrating tablet

Methodology Applied

Scientific EffectCapillary action: Capillary Action

Implementation Method 2

low-substituted hydroxypropyl cellulose... provide a quick disintegrability to the orally disintegrating tablet

Methodology Applied

Scientific EffectSwelling:

Implementation Method 3

D-mannitol, low-substituted hydroxypropyl cellulose... and microcrystalline cellulose... maintains hardness across varying tableting pressures

Methodology Applied

Scientific EffectCrystalline structure:

Implementation Method 4

maintains hardness across varying tableting pressures

Methodology Applied

Scientific EffectCompression: Compression

Implementation Method 5

exhibits improved humidity resistance, preventing significant thickness increase and hardness loss during storage

Methodology Applied

Scientific EffectHydrophobicity: Hydrophobe

Data Source

PatentUS11167031B2Additive composition for orally disintegrating tablet

Publication Date: 2021.11.09 SAWAI PHARMA

AI summary

Provided is a novel additive for an orally disintegrating tablet providing quick disintegrability and tablet hardness to the orally disintegrating tablet, and a producing method therefor. According to an embodiment of the present invention, there is provided an additive for an orally disintegrating tablet characterized by including D-mannitol, low-substituted hydroxypropyl cellulose (however, excluding the low-substituted hydroxypropyl cellulose having a mean particle size of 20 μm or less and a substitution degree of hydroxypropoxy groups of 11%, a mean particle size of 45 μm or less and a substitution degree of hydroxypropoxy groups of 14%, and a mean particle size of 45 μm or less and a substitution degree of hydroxypropoxy groups of 11% and a 90% cumulated particle size of 100 μm or less), crospovidone, and microcrystalline cellulose, wherein the low-substituted hydroxypropyl cellulose and the crospovidone are included in a ratio of 5:4.