Transdermal Cannabidiol Delivery System Bypassing First-Pass Metabolism

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Solution Overview

Problem

Current oral anti-inflammatory drug delivery methods, such as synthetic anti-inflammatory compounds, suffer from side effects like gastric irritation, renal and hepatic failure, and incomplete bioavailability due to first-pass metabolism, and lack effective delivery systems for cannabidiol, which is essential for chronic pain and inflammation management.

Innovation Solution

A transdermal delivery system for synthetic cannabidiol, using transdermal patches or compositions that bypass liver metabolism and gastrointestinal irritation, providing continuous and controlled release of cannabidiol through the skin, reducing dosing frequency and maintaining stable plasma concentrations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If oral anti-inflammatory compounds are used, then pain and inflammation can be treated, but gastric irritation and ulceration occur

Engineering Contradiction:

Improveanti-inflammatory effectivenessVSAvoidgastric irritation

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses the skin and transdermal delivery system as an intermediary route to deliver cannabinoids systemically, avoiding direct contact with the gastric mucosa. The transdermal patch serves as a mediator that bypasses the harmful gastrointestinal pathway while achieving systemic anti-inflammatory effects through cannabinoid receptors.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If oral anti-inflammatory compounds are used, then pain and inflammation can be treated, but renal and hepatic failure may occur

Engineering Contradiction:

Improveanti-inflammatory effectivenessVSAvoidrenal and hepatic toxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The transdermal delivery system acts as an intermediary pathway that bypasses first-pass hepatic metabolism and renal excretion pathways. By delivering cannabinoids through the skin directly into systemic circulation, the patent avoids the toxic metabolic processing that occurs in the liver and kidney when compounds are administered orally.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If oral anti-inflammatory compounds are used, then pain and inflammation can be treated, but incomplete bioavailability occurs due to first-pass metabolism

Engineering Contradiction:

Improveanti-inflammatory effectivenessVSAvoidbioavailability

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The transdermal route serves as an intermediary delivery pathway that circumvents first-pass hepatic metabolism. The skin acts as a portal of entry that allows cannabinoids to enter systemic circulation directly, preserving the full dosage and achieving complete bioavailability without the metabolic loss that occurs with oral administration.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the administration parameter from oral to transdermal, fundamentally altering the absorption pathway. This parameter change eliminates first-pass metabolism and achieves complete bioavailability, allowing the full therapeutic dose of cannabinoids to reach systemic circulation.

Inventive Principle:

Principle #35Parameter changes

4Reliability

If frequent dosing is used to maintain therapeutic levels, then pain and inflammation can be controlled, but patient compliance decreases

Engineering Contradiction:

Improvepain control effectivenessVSAvoiddosing frequency

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The transdermal patch provides continuous release of cannabinoids over an extended period (typically 24-72 hours), maintaining steady therapeutic plasma concentrations without interruption. This continuous delivery eliminates the need for frequent dosing intervals, significantly improving patient compliance while ensuring consistent pain and inflammation control.

Inventive Principle:

Principle #20Continuity of useful action

Solution Approach 2:

The patent applies a single application of the transdermal patch that delivers a sufficient or slightly excessive total dose over an extended period, ensuring therapeutic levels are maintained throughout the wear period. This single application replaces multiple smaller doses, reducing dosing frequency while maintaining or exceeding the cumulative therapeutic effect.

Inventive Principle:

Principle #16Partial or excessive action

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 enhances bioavailability and reduces side effects by delivering cannabidiol directly into systemic circulation, offering prolonged therapeutic effects with reduced dosing frequency and stable plasma concentrations, effectively managing chronic pain and inflammation without the drawbacks of oral routes.

Implementation Method 1

Methodology Applied

Scientific EffectTransdermal delivery: Permeation

Data Source

PatentUS12121617B2Transdermal delivery of cannabidiol

Publication Date: 2024.10.22 PIKE THERAPEUTICS INC

AI summary

Provided is a transdermal drug delivery system comprising cannabidiol, or a cannabidiol salt alone or in combinations thereof. Transdermal delivery can provide a drug plasma concentration at predetermined rate for a predetermined period of time with a simplified therapeutic regimen by decreasing dosing frequency for the treatment and/or prevention of pain and/or inflammation.