Glycerol-Dissolved Cannabinoid Ions for Reduced First-Pass Oxidation
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Solution Overview
Problem
Cannabinoids consumed through conventional routes are oxidized by cytochrome P450 in the lungs and liver, leading to undesirable metabolism and pharmacokinetics.
Innovation Solution
Formulations of cannabinoid ions dissolved in glycerol, which convert to cannabinoid molecules at neutral pH, maximizing surface area and absorption through epithelial tissues to avoid first-pass metabolism.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If cannabinoids are administered through conventional routes (inhalation or oral ingestion), then they are easily absorbed into the bloodstream, but they undergo oxidation by cytochrome P450 in the lungs and liver
Solution Approach 1:
The patent uses glycerol as an intermediary carrier that facilitates the transport of cannabinoid ions through the epithelium while protecting them from immediate oxidation. The glycerol-based formulation acts as a protective medium that allows the cannabinoids to bypass first-pass metabolism in the liver and lungs, thereby reducing cytochrome P450 mediated oxidation while maintaining ease of administration through oral or topical routes
2Productivity
If cannabinoid ions are dissolved in glycerol, then they convert to cannabinoid molecules at neutral pH and absorb rapidly through epithelium, but the cannabinoids become insoluble in both glycerol and bodily fluids
Solution Approach 1:
The patent utilizes pH-dependent parameter changes to control the solubility and absorption characteristics of the cannabinoids. At neutral pH, the cannabinoid ions convert to molecules that are insoluble in glycerol and bodily fluids, causing them to partition out and adhere to the epithelium for rapid absorption. This pH-triggered phase change enables controlled release and enhances absorption rate while managing solubility issues through the glycerol carrier system
3Quantity of substance
If cannabinoids undergo first-pass metabolism in the lungs and liver, then they are metabolized by cytochrome P450, but this reduces the bioavailability and alters pharmacokinetics
Solution Approach 1:
The patent applies preliminary action by formulating cannabinoids as ions dissolved in glycerol before administration, which prevents them from undergoing first-pass metabolism in the lungs and liver. The glycerol-based formulation ensures that the cannabinoids are delivered directly to the target tissues or bloodstream without being prematurely metabolized, thereby preserving bioavailability and controlling the timing of metabolic clearance
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
Minimizes cytochrome P450 mediated oxidation, improving pharmacokinetics by allowing rapid absorption into the bloodstream or skin, thereby reducing metabolic interference.
Implementation Method 1
The administration of cannabinoid ions that are dissolved in glycerol to a human or an animal results in the pH-dependent conversion of the cannabinoid ions into cannabinoid molecules
Implementation Method 2
The cannabinoid molecules then rapidly partition out of the glycerol and adhere to the epithelium where they absorb into the blood
Implementation Method 3
absorb into the blood (during oral administration) or the skin and underlying tissue (during topical administration)
Implementation Method 4
The cannabinoid ions are anions that carry net negative charges that repel each other to maximize their surface area
Data Source
AI summary
Various aspects of this patent document relate to cannabinoid ions that are dissolved in glycerol, in which the cannabinoid ions are not carboxylates. Such compositions are suitable for the oral and topical administration of the cannabinoid ions. Glycerol is more hydrophobic than water, which enables higher concentrations of the cannabinoid ions in glycerol relative to water. Glycerol is also more appealing for oral administration than other hydrophobic solvents such as ethanol.