Self-Emulsifying Cannabinoid Tablets for High Load and Smooth Mouthfeel
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Solution Overview
Problem
Existing carrier systems for gastrointestinal delivery of cannabinoids face challenges such as degradation, low uptake, steric hindrance, unsuitable mouthfeel, and inadequate sensorics properties, particularly when high doses are administered, leading to inefficient and inconvenient delivery.
Innovation Solution
A self-emulsifying system comprising surfactants, lipids, and cannabinoids, stable at pH 1-4, which forms an emulsion upon release in the oral cavity for gastrointestinal delivery, enhancing uptake and stability while improving sensorics.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If carrier systems are used to deliver high doses of cannabinoids, then the cannabinoid load is increased, but the mouthfeel becomes unsuitable (sandy feeling, creaking sound)
Solution Approach 1:
The patent changes the physical state of the carrier system from solid particles to a liquid self-emulsifying system. This parameter change allows high cannabinoid loading while eliminating the sandy feeling and creaking sounds associated with solid carriers, as the liquid system flows smoothly and emulsifies upon contact with saliva.
Solution Approach 2:
The patent uses a composite self-emulsifying system comprising multiple components (surfactants, oils, co-solvents, and cannabinoids) that work together to achieve both high loading capacity and improved mouthfeel. The synergistic interaction between these components allows the system to maintain stability while providing a smooth sensory experience.
2Ease of operation
If carrier systems are released in the oral cavity, then delivery to gastrointestinal tract is enabled, but the carrier systems may be degraded resulting in less uptake
Solution Approach 1:
The patent modifies the chemical composition of the carrier system by incorporating gastroresistant surfactants and stabilizing agents that resist degradation in the gastrointestinal environment. This parameter change ensures the system maintains its integrity during transit through the GI tract, preventing premature breakdown and ensuring efficient cannabinoid uptake.
Solution Approach 2:
The self-emulsifying system acts as an intermediary between the cannabinoid and the gastrointestinal tract. The surfactants and co-solvents in the system protect the cannabinoid from degradation while facilitating its transport and absorption, effectively mediating the interaction between the drug and the biological environment.
3Quantity of substance
If conventional carrier systems are used, then cannabinoids can be contained for delivery, but steric hindrance results in less cell uptake
Solution Approach 1:
The patent changes the size and structure of the carrier system by using a liquid self-emulsifying formulation that forms small micellar structures upon emulsification. This parameter change reduces steric hindrance compared to larger solid carrier particles, allowing better penetration and uptake by intestinal cells while maintaining high cannabinoid containment capacity.
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 system allows high-load, stable delivery of cannabinoids with improved uptake and reduced adverse effects, maintaining high plasma concentrations over time, and enhancing sensorial properties.
Implementation Method 1
self-emulsifying systems including surfactants with a polyethylene glycol moiety... forms an emulsion upon release in the oral cavity
Implementation Method 2
one or more self-emulsifying systems includes i) at least one or more surfactants, one or more lipids
Implementation Method 3
stable at a pH of about 1-4 and being operable to gastrointestinal tract delivery
Data Source
AI summary
An orally dissolvable or chewable tableted powder formulation is presented. The formulation includes one or more carrier systems including one or more liquid or solid self-emulsifying systems loaded with cannabinoids in an amount of at least 10% by weight of the tableted powder formulation. The one or more self-emulsifying systems includes: at least one or more surfactants, one or more lipids and one or more isolated or synthetic cannabinoids when self-emulsifying system is a liquid self-emulsifying system, and at least one or more surfactants, one or more waxes and one or more isolated or synthetic cannabinoids when self-emulsifying system is a solid self-emulsifying system. The formulation further includes one or more water-soluble agents in an amount of 20-80% by weight of the tableted powder formulation and one or more flavors. The one or more surfactants includes one or more surfactants having a chemical structure that includes a polyethylene glycol moiety.