Cannabidiol Oral Formulation with Bile Salts for Epilepsy

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Solution Overview

Problem

Current treatments for epilepsy often have limitations in delivering effective doses of cannabidiol orally, with existing formulations facing challenges in achieving stable plasma levels and potential liver enzyme elevations.

Innovation Solution

The development of compositions comprising cannabidiol, high oleic acid sunflower oil, bile salts, and carriers, specifically formulated to enhance oral bioavailability and stability, while minimizing liver enzyme elevations, by optimizing the ratio of cannabidiol to other components.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral formulations of cannabidiol are used to treat epilepsy, then treatment accessibility is improved, but plasma level stability and bioavailability are insufficient

Engineering Contradiction:
Improveoral delivery accessibilityVSAvoidplasma level stability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent introduces specific formulation intermediaries including bile salts (e.g., cholic acid, deoxycholic acid) and lipids (e.g., phospholipids, triglycerides) that act as carriers and facilitators for cannabidiol absorption. These intermediaries enhance the bioavailability and plasma level stability of cannabidiol when administered orally, resolving the contradiction between oral delivery accessibility and plasma level stability.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies key formulation parameters including the ratio of cannabidiol to formulation components, the type and concentration of bile salts, and the lipid composition. By optimizing these parameters, the formulation achieves enhanced bioavailability and stable plasma levels while maintaining oral delivery convenience.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If higher doses of cannabidiol are administered to achieve effective plasma levels, then treatment efficacy is improved, but liver enzyme elevations occur

Engineering Contradiction:
Improvetreatment efficacyVSAvoidliver enzyme elevations
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses bile salts and lipids as intermediary substances that facilitate cannabidiol absorption and metabolism. These intermediaries enable effective plasma levels to be achieved at lower cannabidiol doses by improving bioavailability, thereby reducing the risk of liver enzyme elevations while maintaining treatment efficacy.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent optimizes the formulation parameters including the concentration of cannabidiol, the type and amount of bile salts, and the lipid composition. By adjusting these parameters, the formulation achieves effective plasma levels with reduced cannabidiol dosage, minimizing liver enzyme elevations while maintaining therapeutic efficacy.

Inventive Principle:
Principle #35Parameter changes

3Ease of manufacture

If conventional oral formulations are used, then manufacturing simplicity is maintained, but bioavailability and steady-state plasma levels are insufficient

Engineering Contradiction:
Improveformulation simplicityVSAvoidbioavailability
Core Design Contradiction:
Ease of manufactureVSQuantity of substance

Solution Approach 1:

The patent creates a composite oral formulation containing cannabidiol combined with bile salts, lipids, and other formulation components in specific ratios. This composite material enhances bioavailability and achieves higher steady-state plasma levels compared to conventional simple oral formulations, while remaining manufacturable using standard pharmaceutical techniques.

Inventive Principle:
Principle #40Composite materials

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 compositions achieve higher steady-state cannabidiol plasma levels and maintain liver enzyme stability, providing effective treatment for epilepsy with improved bioavailability and safety.

Implementation Method 1

The compositions achieve higher steady-state cannabidiol plasma levels... enhancing oral bioavailability

Methodology Applied
Scientific EffectAbsorption: Absorption (physical)

Implementation Method 2

maintain liver enzyme stability... minimizing liver enzyme elevations

Methodology Applied
Scientific EffectEnzyme stabilization: Enzyme

Data Source

PatentUS11931369B1Compositions and methods for treating epilepsy
Publication Date: 2024.03.19 POVIVA CORP
  • US11931369B1 patent drawing
  • US11931369B1 patent drawing
  • US11931369B1 patent drawing

AI summary

Disclosed herein are compositions and methods for delivering compositions to a subject in need of treatment for epilepsy. The disclosed compositions are orally delivered. Further disclosed are kits comprising the disclosed compositions as part of a method of delivering cannabidiol and CBD-containing compositions to subjects in need of treatment for epilepsy.