Micellar Cannabinoid Oral Composition for Solubility and Absorption
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Solution Overview
Problem
Cannabinoids, particularly CBD and THC, have low water solubility and bioavailability, limiting their effective administration and medicinal use due to poor absorption and permeability, necessitating the development of compositions that enhance solubility and bioavailability while being stable, easy to manufacture, and cost-effective.
Innovation Solution
An oral composition comprising a cannabinoid compound, an emulsifier with an HLB value between 10 and 25, an organic acid, and optionally a dextrin compound and silica derivative, which creates a micelle formulation to enhance dissolution and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Device complexity
If cannabinoids are administered orally in standalone form, then the formulation is simple, but the bioavailability is very low due to poor absorption caused by low solubility and low permeability
Solution Approach 1:
The patent applies composite materials by combining cannabinoids with multiple components including phospholipids (e.g., lecithin), surfactants, co-solvents, and cyclodextrins to form a complex delivery system. This composite formulation enhances both solubility and permeability, achieving up to 100 times higher bioavailability compared to standalone cannabinoid compounds while maintaining formulation stability.
Solution Approach 2:
The patent utilizes parameter changes by modifying the physical and chemical properties of the formulation through pH adjustment using acid components (e.g., citric acid, acetic acid) and controlling the hydrophilic-lipophilic balance (HLB) of emulsifiers. These parameter modifications optimize the solubility and absorption characteristics of cannabinoids in the gastrointestinal tract, significantly improving bioavailability.
2Quantity of substance
If acidic environments are used to improve solubility, then the solubility increases, but the cannabinoids degrade and create impurities
Solution Approach 1:
The patent employs phospholipids and surfactants as intermediary substances that form micellar structures to solubilize cannabinoids without requiring strongly acidic environments. These intermediaries create a protective microenvironment that maintains cannabinoid stability while enhancing solubility through micelle formation, avoiding the degradation issues associated with direct acid exposure.
Solution Approach 2:
The patent carefully controls pH parameters within a moderate range (pH 3-7) using weak acid components like citric acid and acetic acid, rather than strong acids. This parameter optimization achieves adequate solubility enhancement while maintaining cannabinoid stability and preventing degradation, balancing solubility improvement with formulation stability.
3Quantity of substance
If emulsifiers with high HLB values are used to enhance solubility, then the solubility improves, but the formulation complexity increases
Solution Approach 1:
The patent selects emulsifiers and phospholipids that perform multiple functions simultaneously: they act as solubility enhancers through micelle formation, serve as stabilizers to prevent cannabinoid degradation, provide permeability enhancement at the intestinal barrier, and contribute to overall formulation stability. This multi-functionality reduces the need for additional separate components, managing formulation complexity while achieving superior solubility.
4Reliability
If alcohol or organic solvents are used to increase bioavailability, then the absorption improves, but the safety and acceptability decrease due to undesirable alcoholic content
Solution Approach 1:
The patent uses phospholipids, surfactants, and co-solvents (such as medium-chain triglycerides and propylene glycol) as intermediary substances to enhance cannabinoid solubility and absorption without requiring alcohol or harmful organic solvents. These intermediaries form micellar structures that facilitate cannabinoid delivery across the intestinal barrier, achieving high bioavailability through safe, food-grade components.
Data Source
AI summary
The present invention is based on the highly soluble and bioavailable cannabinoid compositions which can be made at a commercial scale with a simple manufacturing process. Thus, the present invention relates to oral compositions comprising a cannabinoid compound, for use in the nutraceutical, pharmaceutical, food or beverage industries and its production methods.