Aqueous Oral Cannabinoid Solution Stability and Absorption

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Solution Overview

Problem

Current cannabinoid formulations, such as gelatin capsule dronabinol, are unstable at room temperature and exhibit high inter-subject variability in in vivo absorption, leading to inconsistent drug delivery and faster metabolism.

Innovation Solution

An aqueous-based oral cannabinoid solution comprising water, alcohol, propylene glycol, and a co-solvent like polyethylene glycol, stabilized with antioxidants like butylated hydroxyanisole, which maintains stability at room or refrigerated temperatures and reduces inter-subject variability in absorption.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If gelatin capsule formulations are used, then the cannabinoid can be delivered orally, but the formulation is unstable at room temperature and shows high inter-subject variability in absorption

Engineering Contradiction:
Improveabsorption consistencyVSAvoidformulation stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent changes the physical and chemical parameters of the formulation by transitioning from a gelatin capsule system to an aqueous-based liquid solution with specific solvent compositions (alcohol, propylene glycol, co-solvents). This parameter change enables both improved stability at room temperature and more consistent in vivo absorption by optimizing the solubility and delivery characteristics of the cannabinoid compound.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs a composite formulation system combining multiple components: water as the primary solvent, alcohol for solubility enhancement, propylene glycol as a co-solvent, and additional co-solvents to optimize the pharmaceutical properties. This composite material approach resolves the contradiction by creating a formulation that simultaneously achieves stability and absorption consistency that neither single component could provide alone.

Inventive Principle:
Principle #40Composite materials

2Reliability

If traditional formulations are used, then manufacturing is simpler, but the in vivo absorption shows high inter-subject variability

Engineering Contradiction:
Improveabsorption consistencyVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent optimizes specific formulation parameters including the concentrations of alcohol, propylene glycol, and co-solvents to achieve the desired absorption consistency. By carefully controlling these parameters within specific ranges, the formulation achieves reliable in vivo absorption while maintaining a manufacturable complexity level.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If the solution is made more concentrated to reduce dosing frequency, then the treatment effectiveness improves, but the inter-subject variability in absorption increases

Engineering Contradiction:
Improvedosing efficiencyVSAvoidabsorption consistency
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent optimizes the concentration parameter of the cannabinoid in the aqueous-based solution to achieve an optimal balance. The formulation allows for effective dosing while maintaining consistent absorption across subjects by carefully controlling the concentration within specific ranges and combining it with the optimized solvent system.

Inventive Principle:
Principle #35Parameter changes

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 solution provides a stable and consistent in vivo absorption profile with faster onset and lower variability compared to traditional gelatin capsule formulations, maintaining at least 90% of the active ingredient for extended periods and ensuring effective drug delivery.

Implementation Method 1

An aqueous-based oral cannabinoid solution comprising water, alcohol and propylene glycol that is stable at room or refrigerated temperatures

Methodology Applied
Scientific EffectSolvation: Solvation

Implementation Method 2

stabilized with antioxidants like butylated hydroxyanisole, which maintains stability at room or refrigerated temperatures

Methodology Applied
Scientific EffectOxidation prevention: Oxidation

Data Source

PatentUS10265293B2Oral cannabinoid formulations
Publication Date: 2019.04.23 WELLHOUSE PHARMA LLC

AI summary

Oral cannabinoid formulations, including an aqueous-based oral dronabinol solution, that are stable at room or refrigerated temperatures and may possess improved in vivo absorption profiles with faster onset and lower inter-subject variability.