Lipid-Based Oral Cannabinoid Solution with Ultrahigh Potency Sweeteners

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Solution Overview

Problem

Current cannabinoid formulations face challenges such as poor aqueous solubility, limited bioavailability, and instability, particularly when administered to young children, where low or no ethanol formulations are desirable to avoid adverse effects.

Innovation Solution

A lipid-based oral solution containing a cannabinoid, a lipid solvent, an ultrahigh potency sweetener, and ethanol, characterized by the use of sweeteners like Neotame or Advantame, which provide intense sweetness with reduced ethanol content, making the formulation palatable and stable for young children.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If conventional sweeteners and flavouring agents are used, then the formulation can mask the cannabinoid taste, but these polar substances require polar solvents which are incompatible with lipophilic cannabinoids

Engineering Contradiction:
ImprovepalatabilityVSAvoidsolvent compatibility
Core Design Contradiction:
Ease of operationVSAdaptability or versatility

Solution Approach 1:

The patent uses ultrahigh potency sweeteners that are lipophilic in nature, acting as intermediaries that can dissolve directly in the lipid-based cannabinoid solution without requiring polar solvents. This mediator approach resolves the incompatibility between polar sweeteners and lipophilic cannabinoids while maintaining taste masking capability

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the chemical parameters of the sweetener from polar (conventional) to lipophilic (ultrahigh potency sweeteners like neotame and advantame), enabling direct solubility in lipid-based formulations and eliminating the need for polar solvent systems

Inventive Principle:
Principle #35Parameter changes

2Reliability

If ethanol is included in the formulation, then the cannabinoid remains stable and bioavailable, but high ethanol concentrations are harmful to young children

Engineering Contradiction:
Improvecannabinoid stabilityVSAvoidethanol toxicity to children
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the concentration parameter of ethanol from high levels (conventional formulations) to low levels (less than 10% v/v, preferably less than 5% v/v), maintaining sufficient cannabinoid stability and bioavailability while eliminating harmful effects in pediatric patients

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses ultrahigh potency sweeteners that provide equivalent or superior taste masking to conventional sweeteners at much lower concentrations, allowing the formulation to maintain palatability for children while using minimal ethanol

Inventive Principle:
Principle #26Copying

3Ease of operation

If conventional sweeteners are used, then the formulation can be palatable, but large volumes of polar solvent are required which is impractical for pediatric administration

Engineering Contradiction:
ImprovepalatabilityVSAvoidformulation volume
Core Design Contradiction:
Ease of operationVSVolume of moving object

Solution Approach 1:

The patent changes the sweetness intensity parameter by using ultrahigh potency sweeteners with sweetness intensities greater than 750 times that of sucrose, enabling effective taste masking in small volumes suitable for pediatric administration

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention applies local quality by concentrating the sweetening function in ultrahigh potency sweeteners that can be effectively dissolved in the lipid phase, providing localized taste masking without requiring bulk polar solvent

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS12213985B2Oral cannabinoid formulations
Publication Date: 2025.02.04 JAZZ PHARM RES UK LTD

AI summary

The present invention relates to a cannabinoid containing oral solution. Preferably the oral solution comprises a cannabinoid, a lipid solvent, a sweetener and ethanol, characterised in that the sweetener is an ultrahigh potency sweetener.