Three-Layer Tablet Segregating Cetirizine from Pseudoephedrine

Solution Overview

Problem

Combining antihistamine cetirizine, nasal decongestant pseudoephedrine, and analgesic naproxen in a single tablet is challenging due to differences in their 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 three-layer tablet design where naproxen, pseudoephedrine, and cetirizine are separated into distinct layers, with pseudoephedrine in a sustained release layer to maintain therapeutic effectiveness for at least twelve hours, using granulation and dry blending processes to prepare each layer, ensuring they are not in direct contact to prevent degradation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If cetirizine, pseudoephedrine, and naproxen are combined in a single tablet, then all three symptoms (allergy, congestion, headache) can be treated simultaneously, but cetirizine degrades in the physical presence of pseudoephedrine and naproxen

Engineering Contradiction:

Improveability to treat multiple symptomsVSAvoidstability of cetirizine

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The tablet is divided into three distinct layers: a first layer containing naproxen, a second layer containing pseudoephedrine, and a third layer containing cetirizine. This segmentation physically separates cetirizine from the other two ingredients that cause its degradation, while still allowing all three medications to be delivered in a single tablet that treats multiple symptoms simultaneously.

Inventive Principle:

Principle #1Segmentation

2Duration of action of moving object

If pharmaceutically active agents with different durations of action are combined, then extended treatment coverage is achieved, but extended release modifications are required which complicates formulation

Engineering Contradiction:

Improveduration of symptom reliefVSAvoidformulation complexity

Core Design Contradiction:

Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The tablet is divided into three distinct layers: a first layer containing naproxen, a second layer containing pseudoephedrine, and a third layer containing cetirizine. This segmentation physically separates cetirizine from the other two ingredients that cause its degradation, while still allowing all three medications to be delivered in a single tablet that treats multiple symptoms simultaneously.

Inventive Principle:

Principle #1Segmentation

3Ease of operation

If multiple pharmaceutically active agents are combined in a single tablet, then convenience of administration is improved, but manufacturing difficulties arise due to incompatibility and different release requirements

Engineering Contradiction:

Improveconvenience of administrationVSAvoidmanufacturing difficulty

Core Design Contradiction:

Ease of operationVSEase of manufacture

Solution Approach 1:

The tablet is divided into three distinct layers: a first layer containing naproxen, a second layer containing pseudoephedrine, and a third layer containing cetirizine. This segmentation physically separates cetirizine from the other two ingredients that cause its degradation, while still allowing all three medications to be delivered in a single tablet that treats multiple symptoms simultaneously.

Inventive Principle:

Principle #1Segmentation

Data Source

PatentUS8246988B2Three layer tablet containing cetirizine, pseudoephedrine, and naproxen

Publication Date: 2012.08.21 KENVUE BRANDS LLC

AI summary

In one aspect, the present invention features a tablet including a first drug layer, a second drug layer, and a third drug layer, wherein (i) the first drug layer includes naproxen; (ii) a second drug layer including pseudoephedrine; and (iii) the third drug layer includes cetirizine; wherein the first drug layer is in contact with the second drug layer, the third drug layer is in contact with the second drug layer, and the first drug layer is not in contact with the third drug layer, and wherein the 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.