Transdermal CBD Patch Bypassing First-Pass Metabolism
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current methods for delivering cannabidiol (CBD) for seizure disorders, such as Epidiolex, face challenges including high discontinuation rates due to side effects like hepatocellular injury and somnolence, and impractical patch sizes for transdermal delivery systems, as well as the use of psychoactive THC, which complicates therapeutic efficacy and patient compliance.
Innovation Solution
A transdermal delivery system using highly purified synthetic CBD, formulated as a transdermal patch or liquid formulation, providing a controlled release of CBD directly into systemic circulation, avoiding first-pass metabolism and gastrointestinal irritation, with a focus on reducing dosing frequency and minimizing side effects through sustained plasma concentration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral CBD formulations (Epidiolex) are used to treat seizure disorders, then therapeutic efficacy is achieved, but discontinuation rates increase due to side effects like hepatocellular injury and somnolence
Solution Approach 1:
The patent introduces a transdermal delivery system as an intermediary between the CBD and the patient's systemic circulation, bypassing the gastrointestinal tract and liver. This mediator approach allows CBD to reach the bloodstream directly through the skin, maintaining therapeutic efficacy while avoiding hepatocellular injury and reducing first-pass metabolism-related side effects
Solution Approach 2:
The patent replaces the oral administration route (mechanical swallowing and gastrointestinal processing) with a transdermal delivery system. This substitution eliminates the need for gastrointestinal digestion and hepatic first-pass metabolism, thereby reducing side effects while maintaining drug delivery effectiveness
2Reliability
If transdermal delivery systems are used to deliver CBD, then first-pass metabolism is avoided, but patch sizes become impractically large
Solution Approach 1:
The patent optimizes the formulation parameters of the transdermal delivery system, including the use of specific penetration enhancers, adhesive compositions, and CBD concentrations. By changing these parameters, the system achieves effective drug delivery through the skin at practical patch sizes, avoiding the need for excessively large application areas while maintaining the advantage of bypassing first-pass metabolism
3Manufacturing precision
If highly purified synthetic CBD is used in transdermal formulations, then therapeutic precision is improved, but formulation complexity increases
Solution Approach 1:
The patent extracts and isolates highly purified synthetic CBD from complex plant extracts, removing unwanted constituents such as THC and other cannabinoids. This extraction process produces a purified active ingredient that can be formulated into transdermal systems with controlled complexity, achieving manufacturing precision while managing formulation complexity through selective isolation of the therapeutic component
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 system effectively reduces seizure frequency by maintaining consistent CBD levels, improving therapeutic efficacy, enhancing patient compliance, and reducing side effects, while providing a controlled and sustained release of CBD for extended periods.
Implementation Method 1
A transdermal delivery system using highly purified synthetic CBD, formulated as a transdermal patch or liquid formulation, providing a controlled release of CBD directly into systemic circulation
Implementation Method 2
providing a controlled release of CBD directly into systemic circulation, avoiding first-pass metabolism and gastrointestinal irritation, with a focus on reducing dosing frequency and minimizing side effects through sustained plasma concentration
Data Source
AI summary
The present disclosure relates to the transdermal administration of cannabidiol (CBD) for the reduction of seizure frequency in the treatment of “treatment-resistant epilepsy” (TRE).