Cannabinoid Receptor Ligands for Controlled Dosing and Bioavailability
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Solution Overview
Problem
Existing methods for using cannabinoids for medicinal purposes, such as smoking cannabis, suffer from disadvantages including the presence of carcinogens and toxins, difficulty in maintaining proper dosing, and low bioavailability of active ingredients, while extraction processes struggle to isolate individual cannabinoids at high purity.
Innovation Solution
Development of novel cannabinoid receptor ligands, represented by compounds of formula (I), which can act as ligands to cannabinoid receptors and are used in pharmaceutical compositions for treating various diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If cannabis is smoked for medicinal purposes, then cannabinoids are delivered to patients, but carcinogens and toxins are introduced causing lung damage
Solution Approach 1:
The patent extracts and isolates specific cannabinoids from the complex cannabis plant matrix, separating the beneficial active ingredients from harmful constituents like carcinogens and toxins. This extraction process produces purified cannabinoid compounds that can be delivered without the harmful smoke components.
Solution Approach 2:
The patent introduces pharmaceutical compositions and delivery systems as intermediaries between the cannabis source and the patient. These compositions include purified cannabinoids combined with safe carriers and excipients, serving as a mediator that delivers therapeutic effects without introducing carcinogenic smoke.
2Quantity of substance
If plant-based cannabis is used, then natural cannabinoids are available, but dosing control is difficult due to variability in plant strains and growing conditions
Solution Approach 1:
The patent applies parameter changes by standardizing the chemical composition through purification and formulation processes. By controlling parameters such as cannabinoid concentration, purity levels, and composition ratios in the pharmaceutical composition, consistent dosing is achieved regardless of natural plant variability.
Solution Approach 2:
The patent performs preliminary action by pre-analyzing and standardizing the cannabinoid content during the pharmaceutical composition development phase. This includes establishing precise formulations with defined cannabinoid ratios and concentrations before clinical use, ensuring dosing consistency from the outset.
3Quantity of substance
If smoking is used as delivery method, then cannabinoids reach the patient, but bioavailability is relatively low compared to other delivery methods
Solution Approach 1:
The patent changes the physical and chemical parameters of cannabinoid delivery by transitioning from inhalation to alternative routes such as oral, sublingual, or transdermal administration. This involves modifying the pharmaceutical composition to include appropriate excipients, carriers, and formulation technologies that enhance absorption and bioavailability through the selected delivery route.
Data Source
AI summary
The present application discloses a compound of formula (I), compositions comprising said compound, and a method of using said compound as a cannabinoid receptor ligand in the treatment or prevention of diseases associated with a cannabinoid receptor, such as, CB1, CB2, 5HT1A, 5HT2A, GPR18, GPR119, TRPV1, TPRV2, PPARγ or a μ-opioid receptor.