Dextromethorphan Transdermal Patch Adhesive Design
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Solution Overview
Problem
Current methods for delivering dextromethorphan, such as NUEDEXTA, require co-administration of a CYP2D6 inhibitor like quinidine and have unpredictable dosing due to first-pass metabolism, leading to potential side effects and inefficiencies.
Innovation Solution
Development of transdermal delivery devices with a patch design featuring an adhesive layer and a reservoir layer containing dextromethorphan, which includes a skin permeation enhancer to achieve higher flux and sustained release profiles, allowing for effective plasma concentration without quinidine co-administration, suitable for various dosing frequencies.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral administration of dextromethorphan is used, then the drug can be delivered systemically, but first-pass metabolism causes unpredictable dosing and requires co-administration of CYP2D6 inhibitors
Solution Approach 1:
The patent extracts dextromethorphan from the oral administration route and delivers it directly through the skin via transdermal patch, eliminating first-pass metabolism and the need for CYP2D6 inhibitors like quinidine, thereby resolving the contradiction between dosing predictability and treatment complexity
Solution Approach 2:
The patent introduces a transdermal patch as an intermediary delivery system that bypasses the gastrointestinal tract and liver metabolism, allowing dextromethorphan to enter systemic circulation directly through the skin, thus achieving predictable dosing without additional medications
2Productivity
If transdermal delivery with skin permeation enhancer is used, then flux and bioavailability are improved, but potential skin irritation may occur
Solution Approach 1:
The patent modifies the chemical parameters of the adhesive layer by incorporating specific skin permeation enhancers (oleic acid, isopropyl myristate, or propylene glycol) at optimized concentrations, which increase drug flux while the adhesive matrix controls the rate of enhancement to minimize skin irritation
Solution Approach 2:
The patent creates a composite adhesive layer combining polymer adhesive with skin permeation enhancers, where the composite structure provides both the necessary drug delivery enhancement and controlled release properties to balance flux improvement with skin tolerance
3Reliability
If frequent dosing is required to maintain therapeutic levels, then plasma concentration is maintained, but patient compliance decreases
Solution Approach 1:
The patent implements continuous drug delivery through the transdermal patch, maintaining steady plasma concentrations of dextromethorphan over extended periods (7-14 days), which eliminates the need for frequent dosing and significantly improves patient compliance while keeping therapeutic levels consistent
4Quantity of substance
If higher concentration of dextromethorphan is used in the reservoir layer, then therapeutic effect is enhanced, but risk of side effects increases
Solution Approach 1:
The patent creates a dynamic delivery system where the adhesive layer gradually releases dextromethorphan into the skin over time, preventing sudden high concentrations and allowing the body to process the drug at manageable rates, thus reducing side effects while maintaining therapeutic effectiveness
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 transdermal delivery devices provide a therapeutically effective plasma concentration of dextromethorphan with reduced side effects and improved patient compliance by avoiding first-pass metabolism and allowing for less frequent dosing, while being effective for neurological disorders like pseudobulbar affect.
Implementation Method 1
The adhesive layer can comprise dextromethorphan dispersed in an adhesive, and a skin permeation enhancer
Data Source
AI summary
Provided herein are transdermal delivery devices comprising dextromethorphan. The transdermal delivery device can be characterized by the novel design, for example, with an adhesive layer and a reservoir layer, with an adhesive layer comprising a mixture of two adhesives, and/or with a skin permeation enhancer, e.g., in an amount that can significantly enhance the flux of dextromethorphan. The transdermal delivery device can also be characterized by its in vitro and/or in vivo release profile, for example, that can provide a desired pharmacokinetic profile described herein. Also provided herein are methods of administering dextromethorphan, and methods of treating a disease or disorder described herein, using the transdermal delivery device herein.