Ketoprofen Water-Based Patch Using Amine Solubilizer
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Solution Overview
Problem
Water-based patches containing ketoprofen face challenges with low storage stability and transdermal absorbability due to the low water solubility of ketoprofen and esterification reactions with polyhydric alcohols, while oil-based patches can provide high absorbability but cause skin irritation.
Innovation Solution
A water-based patch using an amine, specifically diisopropanolamine, as a solubilizer for ketoprofen, dissolved in a polyethylene glycol base to enhance stability and absorbability, with optimal weight percentages of ketoprofen, amine, and polyethylene glycol to prevent skin irritation and maintain patch properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If polyhydric alcohol (e.g., glycerin) is used as a solubilizer in water-based patches, then transdermal absorbability is improved, but storage stability deteriorates due to esterification reaction with ketoprofen
Solution Approach 1:
The invention changes the chemical parameters by replacing polyhydric alcohols with specific amines (diisopropanolamine, diethanolamine, triethanolamine) that have different chemical properties - they solubilize ketoprofen effectively but do not undergo esterification reactions, thus improving storage stability while maintaining transdermal absorbability
Solution Approach 2:
The amine acts as an intermediary solubilizer that bridges the compatibility between water-based patch matrix and ketoprofen, providing both solubility enhancement and chemical stability without the harmful esterification side reaction that occurs with polyhydric alcohols
2Stability of the object's composition
If oil-based patch base is used, then storage stability is improved, but skin irritation occurs
Solution Approach 1:
The invention changes the base composition parameters by using water-based matrix with specific amine solubilizers instead of oil-based matrices, achieving both chemical stability and skin compatibility by eliminating irritating oil components while maintaining drug stability through amine-ketoprofen complexes
3Stability of the object's composition
If ketoprofen is dispersed in the patch base, then storage stability is improved, but transdermal absorbability is reduced
Solution Approach 1:
The invention changes the physical state parameter of ketoprofen from dispersed solid particles to dissolved molecular state by using amines as solubilizers, creating a homogeneous solution that enhances both storage stability (preventing crystallization) and transdermal absorbability (improving drug availability)
4Reliability
If specific solubilizers (crotamiton, fatty acid esters, essential oils) are added to water-based patches, then transdermal absorbability is improved, but production complexity increases
Solution Approach 1:
The invention changes the solubilizer selection parameters by choosing amines (diisopropanolamine, diethanolamine, triethanolamine) that are water-soluble and chemically compatible with the patch matrix, eliminating the need for complex production controls required for lipophilic solubilizers and simplifying the manufacturing process
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 patch achieves high transdermal absorbability and storage stability with low skin irritability, outperforming conventional patches in both aspects.
Implementation Method 1
an amine which serves as a solvent capable of dissolving a large amount of ketoprofen as a solubilizer for the main drug
Implementation Method 2
dissolving the ketoprofen in a water-based base containing polyethylene glycol having weak interaction with the ketoprofen
Implementation Method 3
an esterification reaction proceeds between the ketoprofen and a solubilizer having a hydroxyl group such as a polyhydric alcohol... This results in a problem of low storage stability
Data Source
AI summary
Provided is a water-based patch that contains ketoprofen as an active ingredient, provides high transdermal absorbability of the ketoprofen, and has high safety and high storage stability. The water-based patch contains the ketoprofen, an amine, and polyethylene glycol. In the water-based patch, the added amount of the ketoprofen in a paste is 0.1 to 5% by weight, the added amount of the amine in the paste is 0.5 to 10% by weight, and the added amount of the polyethylene glycol in the paste is 5 to 30% by weight. Particularly, in the water-based patch, diisopropanolamine is used as the amine.