Coated Rapid-Disintegrating Tablets with Mannitol-Croscarmellose Core

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Solution Overview

Problem

Existing rapidly disintegrating tablets face challenges with low hardness and high abrasion, making them unsuitable for coating and storage, which can lead to inconsistent dosing and reduced shelf life due to moisture sensitivity and increased disintegration times.

Innovation Solution

A pharmaceutical formulation comprising a homogenized co-mixture of spray-granulated mannitol and cross-linked croscarmellose sodium, combined with an active pharmaceutical ingredient, and a coating solution applied in water or water-ethanol, which enhances mechanical strength and rapid disintegration while maintaining stability under moisture.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If rapidly disintegrating tablet formulations are used, then disintegration speed is improved, but mechanical strength and hardness deteriorate

Engineering Contradiction:

Improvedisintegration speedVSAvoidmechanical strength

Core Design Contradiction:

SpeedVSStrength

Solution Approach 1:

The patent uses a composite excipient system combining mannitol (90-95 wt%) with cross-linked croscarmellose sodium (3-7 wt%) to create a material that exhibits both rapid disintegration properties and sufficient mechanical strength for coating and handling. This composite approach allows the tablet to achieve fast disintegration while maintaining the hardness needed for subsequent processing steps.

Inventive Principle:

Principle #40Composite materials

2Object-affected harmful factors

If coating is applied to protect tablets, then protection against external influences is improved, but disintegration time increases

Engineering Contradiction:

Improveprotection against external influencesVSAvoiddisintegration time

Core Design Contradiction:

Object-affected harmful factorsVSLoss of time

Solution Approach 1:

The patent modifies the coating formulation by incorporating specific amounts of plasticizers (glycerol 10-30 wt%, propylene glycol 10-30 wt%) and surfactants (0.1-5 wt%) to change the coating's physical parameters. These parameter changes make the coating more flexible and permeable, allowing it to provide protection while still permitting rapid moisture penetration and disintegration within 30 seconds.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs a thin film coating (1-5 µm thickness) that provides protective barriers against moisture and external influences while maintaining flexibility. The coating film is designed to be thin enough to allow rapid disintegration while still providing the necessary protection during storage and handling.

Inventive Principle:

Principle #30Flexible shells and thin films

3Speed

If low hardness tablets are produced for rapid disintegration, then disintegration is improved, but abrasion increases

Engineering Contradiction:

Improvedisintegration speedVSAvoidabrasion

Core Design Contradiction:

SpeedVSObject-generated harmful factors

Solution Approach 1:

The patent creates a composite excipient mixture where cross-linked croscarmellose sodium (3-7 wt%) provides structural integrity and reduced abrasion, while mannitol (90-95 wt%) ensures rapid disintegration. This composite material achieves low abrasion (≤0.5%) while maintaining fast disintegration properties.

Inventive Principle:

Principle #40Composite materials

4Strength

If coating is applied to increase hardness, then mechanical strength is improved, but coating evenness deteriorates due to high abrasion

Engineering Contradiction:

Improvemechanical strengthVSAvoidcoating evenness

Core Design Contradiction:

StrengthVSManufacturing precision

Solution Approach 1:

The patent uses a composite excipient system that inherently reduces abrasion through the synergistic combination of mannitol and cross-linked croscarmellose sodium. This low-abrasion property ensures that tablet surfaces remain intact during coating, allowing for even and uniform coating application without surface degradation.

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 formulation achieves tablets with high mechanical strength, low abrasion, and rapid disintegration in the mouth, while maintaining storage stability and allowing for even coating, ensuring consistent dosing and prolonged shelf life.

Implementation Method 1

The smooth surface formed by the coating, together with the choice of a convenient form, can make it easier to take the tablets

Methodology Applied

Scientific EffectFilm formation:

Implementation Method 2

the film or coating is at least partially in the oral cavity in the presence of moisture, leaving the tablet core accessible to moisture and disintegrating rapidly as desired

Methodology Applied

Scientific EffectDissolution:

Implementation Method 3

a homogenized, directly compressible co-mixture of spray-granulated mannitol and cross-linked croscarmellose sodium

Methodology Applied

Scientific EffectSpray granulation:

Data Source

PatentEP2844234B1Tablets with coating and the production thereof

Publication Date: 2020.01.08 MERCK PATENT GMBH

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AI summary

The present invention provides a rapidly disintegrating pharmaceutical formulation in the form of a tablet provided with a coating which has increased mechanical strength or hardness. The invention further relates to the production of said coated tablets and to the use of said formulations.