Multi-Layer Tablet with Coated Drug Particles

Solution Overview

Problem

Combining antihistamine cetirizine, nasal decongestant pseudoephedrine, and analgesic naproxen into a single tablet is challenging due to differences in duration of action and incompatibility, with cetirizine degrading in the presence of pseudoephedrine and naproxen, making it difficult to create a formulation that effectively treats upper respiratory allergy symptoms for an extended period.

Innovation Solution

A tablet design featuring a first drug layer with immediate release coatings of naproxen and cetirizine, and a second sustained release layer of pseudoephedrine, manufactured through granulation and coating processes, to provide therapeutic relief for at least twelve hours.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If multiple pharmaceutically active agents (cetirizine, pseudoephedrine, naproxen) are combined into a single tablet, then the convenience of taking multiple medications is improved, but drug incompatibility and degradation occur

Engineering Contradiction:

Improveconvenience of taking multiple medicationsVSAvoiddrug stability and compatibility

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The tablet is divided into multiple separate layers, each containing different pharmaceutically active agents. The first layer contains cetirizine with immediate release coating, the second layer contains naproxen with immediate release coating, and the third layer contains pseudoephedrine as sustained release layer. This segmentation prevents direct contact between incompatible drugs while maintaining a single-tablet format for convenience.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

Immediate release coatings are applied to the cetirizine and naproxen particles to create a protective barrier. These coatings act as intermediaries that prevent direct interaction between incompatible drugs during manufacturing and storage, while still allowing rapid drug release in the gastrointestinal tract when needed.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Duration of action of moving object

If extended release formulation is used for pseudoephedrine, then the duration of action is improved, but manufacturing complexity increases

Engineering Contradiction:

Improveduration of pseudoephedrine actionVSAvoidtablet structure complexity

Core Design Contradiction:

Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The tablet is divided into multiple separate layers, each containing different pharmaceutically active agents. The first layer contains cetirizine with immediate release coating, the second layer contains naproxen with immediate release coating, and the third layer contains pseudoephedrine as sustained release layer. This segmentation prevents direct contact between incompatible drugs while maintaining a single-tablet format for convenience.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

Different release characteristics are applied to different drug layers. The immediate release coating on cetirizine and naproxen particles provides rapid dissolution, while the sustained release matrix in the pseudoephedrine layer provides extended release. This parameter differentiation achieves extended duration of action without requiring complex controlled-release mechanisms throughout the entire tablet.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If immediate release coating is applied to cetirizine and naproxen particles, then drug compatibility is improved, but manufacturing steps increase

Engineering Contradiction:

Improvedrug compatibilityVSAvoidmanufacturing process simplicity

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

Immediate release coatings are applied to the cetirizine and naproxen particles to create a protective barrier. These coatings act as intermediaries that prevent direct interaction between incompatible drugs during manufacturing and storage, while still allowing rapid drug release in the gastrointestinal tract when needed.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The coating process for cetirizine and naproxen particles is combined into a single manufacturing step, and the layering of multiple drug layers is performed in sequence within an integrated tablet compression process. This merging of operations reduces the overall manufacturing complexity despite the additional coating step.

Inventive Principle:

Principle #5Merging (Combining)

Data Source

PatentUS8252330B2Tablet containing coated particles of cetirizine, pseudoephedrine, and/or naproxen

Publication Date: 2012.08.28 KENVUE BRANDS LLC

AI summary

In one aspect, the present invention features a tablet including a first drug layer and a second drug layer, wherein: (i) the first drug layer includes first drug particles including naproxen and third drug particles including cetirizine, where the first drug particles and/or the third drug particles are coated with an immediate release coating; and (ii) the second drug layer including pseudoephedrine, wherein said second drug layer is a sustained release layer adapted to deliver a therapeutically effective amount of pseudoephedrine for a period of at least twelve hours.