Free Ropinirole Adhesive Patch Stability
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Solution Overview
Problem
Transdermal absorption preparations using acid addition salts of ropinirole have lower permeability and stability issues due to incomplete conversion and potential metal salt precipitation, leading to skin irritation and physical deterioration of patches.
Innovation Solution
A transdermal absorption patch with an acrylic-based adhesive containing no cross-linking agent, hydroxyl or pyrrolidone groups, and free ropinirole, optionally enhanced with transdermal absorption enhancers, antioxidants, and other additives, ensuring complete dissolution and stability of the drug.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If acid addition salt of ropinirole is used in transdermal absorption preparation, then stability and handleability are improved, but transdermal absorbability is significantly reduced
Solution Approach 1:
The invention changes the chemical form parameter of ropinirole from acid addition salt to free base form, enabling high transdermal absorbability while maintaining stability through specific adhesive base composition (acrylic polymer with hydroxyl or carboxyl groups)
Solution Approach 2:
The acrylic-based adhesive base acts as an intermediary medium that facilitates the conversion and stabilization of ropinirole free base, enabling it to maintain stability during storage while achieving high transdermal absorption
2Productivity
If dehydrochlorinating agent is used to convert acid addition salt to free ropinirole, then transdermal absorbability is improved, but the amount of drug in adhesive base is limited and conversion is incomplete
Solution Approach 1:
The invention performs preliminary action by directly using free ropinirole base form in the formulation, avoiding the need for dehydrochlorinating agents and ensuring complete drug availability from the start
3Productivity
If dehydrochlorinating agent is used for conversion, then free ropinirole is generated, but metal salt precipitates causing physical deterioration and skin irritation
Solution Approach 1:
The invention extracts and eliminates the need for dehydrochlorinating agents and metal salts by directly formulating with free ropinirole base, removing the source of metal salt precipitation and associated harmful effects
Solution Approach 2:
The invention converts the potential harm of metal salt precipitation into benefit by using an acrylic-based adhesive base that chelates or complexes with any residual metal ions, preventing precipitation while maintaining drug stability
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 stability of free ropinirole, effectively treating Parkinson's disease with improved drug release and skin compatibility.
Implementation Method 1
the adhesive base consists of (1) an acrylic-based adhesive containing no cross-linking agent, having no carboxyl group and having a hydroxyl group or a pyrrolidone group, (2) free ropinirole
Implementation Method 2
one or more component(s) selected from the group consisting of a transdermal absorption enhancer
Data Source
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AI summary
Provided is an adhesive patch containing ropinirole serving as a therapeutic drug for Parkinson's disease, with the ropinirole used being free ropinirole (ropinirole in free form) added to an adhesive base, wherein the patch exhibits favorable drug permeability and excellent drug stability. Also provided is a transdermal absorption patch using, as an adhesive base, an acrylic-based adhesive having no specific carboxyl group and having a hydroxyl group or a pyrrolidone group, with the patch including free ropinirole added to the adhesive base. Further provided is a ropinirole-containing transdermal absorption patch including a transdermal absorption promoting agent.