Single-Layer Cetirizine Chewable Tablets with Polyol Stability
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Solution Overview
Problem
Cetirizine, an H1-receptor antagonist, is susceptible to degradation when formulated with polyols in conventional tablets, leading to undesired reaction products, and existing bilayer tablets are cumbersome for patients with swallowing difficulties.
Innovation Solution
A single layer chewable tablet formulation comprising cetirizine, an optical isomer, or a pharmaceutically active salt thereof, and at least one polyol, stabilized by cyclodextrin and starch, which maintains chemical and physical stability under various humidity conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If cetirizine is formulated with polyols in conventional tablets, then the tablet provides bulk filling and sweetening, but cetirizine degrades through esterification with polyols
Solution Approach 1:
The patent divides the tablet into two separate layers: a first layer containing cetirizine and a second layer containing polyols. This physical separation prevents esterification between cetirizine and polyols while still allowing both components to fulfill their respective functions in the final tablet product.
Solution Approach 2:
The patent introduces a coating layer as an intermediary barrier between the cetirizine-containing first layer and the polyol-containing second layer. This coating prevents direct contact and chemical reaction between cetirizine and polyols, maintaining chemical stability while allowing both substances to be present in the tablet.
2Reliability
If a bilayer tablet structure is used to separate cetirizine and polyols, then chemical stability is improved, but the tablet becomes cumbersome for patients with swallowing difficulties
Solution Approach 1:
The patent combines the separation function and the chewable function into a single integrated layer structure. The first layer contains both cetirizine and polyols in a mixed formulation that is physically stable, allowing the entire tablet to be chewable and easy to handle while maintaining chemical stability through controlled interaction between the components.
Solution Approach 2:
The patent changes the physical state and interaction parameters of the cetirizine-polyol mixture to create a stable mixed formulation. By adjusting the ratio, molecular weight, and physical form of the polyols, the patent achieves a mixture that remains stable during tablet formation and storage while providing the desired chewable properties.
3Quantity of substance
If polyols of low molecular weight are used in high molar ratios with cetirizine, then the tablet provides adequate bulk filling, but undesired reaction products are formed
Solution Approach 1:
The patent segments the tablet into distinct layers for cetirizine and polyols, preventing the high molar ratio contact that leads to undesired esterification products. This physical separation allows adequate bulk filling with polyols without forming harmful reaction products.
Solution Approach 2:
The patent converts the potential harm of polyol-cetirizine interaction into a benefit by using the controlled interaction in the first layer to create a stable mixed formulation that provides both bulk filling and taste masking, while the second layer provides additional polyol content without risk of reaction.
Data Source
AI summary
The present invention relates to a single layer chewable tablet comprising cetirizine, an optical isomer, or a pharmaceutically active salt thereof and at least one polyol. The present invention also relates to a method of alleviating a sign or symptom of allergy by orally administering the same single layer chewable tablet.