Asenapine Patch Adhesive Composition to Reduce Drug Degradation
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Solution Overview
Problem
The degradation of asenapine during the manufacturing of patches containing an adhesive layer is a challenge, particularly when using asenapine free base, due to factors like contact with other components, heating, or exposure to light.
Innovation Solution
The method involves using an adhesive layer comprising an acid addition salt of asenapine and a desalting agent, such as alkali metal hydroxides or alkaline-earth metal salts, along with a (meth)acrylic acid ester polymer, while excluding rubber adhesives, to reduce degradation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If asenapine free base is used in the adhesive layer, then skin permeability of asenapine is improved, but degradation of asenapine occurs easily during manufacturing
Solution Approach 1:
The patent changes the chemical state of asenapine from free base to acid addition salt form in the adhesive layer, which fundamentally alters its stability characteristics while maintaining skin permeability through the desalting agent mechanism
Solution Approach 2:
The desalting agent acts as an intermediary substance that converts the acid addition salt of asenapine back to the free base form at the skin interface, enabling the free base to achieve skin permeability while the salt form provides manufacturing stability
2Reliability
If asenapine free base is used in the adhesive layer, then drug efficacy is improved, but degradation products are produced during manufacturing
Solution Approach 1:
The patent changes the chemical state of asenapine from free base to acid addition salt form, which prevents degradation during manufacturing while the desalting agent ensures drug efficacy is maintained at the application site
Solution Approach 2:
The patent converts the potentially harmful degradation issue into a benefit by using the acid addition salt form that is stable during manufacturing, while the desalting agent ensures the active drug form is released for efficacy
3Strength
If rubber adhesive is used in the patch, then adhesive property is maintained, but degradation of asenapine is hardly observed (indicating rubber adhesive may protect from degradation)
Solution Approach 1:
The patent changes the chemical state of asenapine to acid addition salt form, which provides inherent stability against degradation without relying on rubber adhesive protection
Solution Approach 2:
The patent extracts the degradation protection function from the rubber adhesive material itself and transfers it to the chemical form of asenapine (acid addition salt), allowing the use of non-rubber adhesives
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
This approach significantly reduces the production of degradation products of asenapine, maintaining the integrity and effectiveness of the patch.
Implementation Method 1
an adhesive composition comprising an acid addition salt of asenapine and a desalting agent
Data Source
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AI summary
The present invention provides a method for manufacturing a patch comprising a backing and an adhesive layer laminated on the backing, comprising: a step of mixing an acid addition salt of asenapine, a (meth)acrylic acid ester (co)polymer and a desalting agent to obtain an adhesive composition; and a step of shaping the adhesive composition to obtain the adhesive layer.