Non-euphoric Cannabinoid Solid Dispersion via Hot Melt Extrusion
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Solution Overview
Problem
Current formulations of natural or synthetic non-euphoric cannabinoids have low solubility and bioavailability due to their insolubility in water and poor dispersion in aqueous phases, leading to inadequate bioavailability and stability issues.
Innovation Solution
A composition comprising a friable/brittle thermoformed extrudate with non-euphoric cannabinoids combined with carriers like amino acids, peptides, proteins, saccharides, and lipids, using hot melt extrusion to create a solid dispersion that enhances solubility and bioavailability, and is stable over time.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If non-euphoric cannabinoids are used in current formulations, then therapeutic effects are achieved, but solubility and bioavailability are too low
Solution Approach 1:
The patent changes the physical-chemical parameters of the cannabinoid formulation by converting crystalline cannabinoids into amorphous form through hot melt extrusion processing. This parameter change increases solubility and bioavailability while maintaining therapeutic efficacy. The amorphous state has higher free energy and better solvation properties compared to the crystalline state.
Solution Approach 2:
The patent creates a composite material system by combining non-euphoric cannabinoids with excipients (such as hydrophilic polymers, surfactants, or lipids) in a matrix. This composite approach enhances the solubility and dispersion of the hydrophobic cannabinoids in aqueous environments, thereby improving bioavailability while preserving therapeutic effects.
2Reliability
If non-euphoric cannabinoids are used in current formulations, then therapeutic effects are achieved, but dispersion in aqueous phase is insufficient
Solution Approach 1:
The patent introduces intermediary substances (excipients such as hydrophilic polymers, surfactants, or lipids) that act as mediators between the hydrophobic cannabinoids and the aqueous environment. These intermediaries enhance wetting, solubilization, and dispersion stability, allowing the cannabinoids to remain uniformly distributed in aqueous phases without compromising therapeutic efficacy.
3Ease of manufacture
If conventional formulation methods are used, then manufacturing is simple, but solubility and bioavailability are inadequate
Solution Approach 1:
The patent employs hot melt extrusion processing to change the physical state of cannabinoids from crystalline to amorphous. This manufacturing technique, while requiring controlled temperature and processing parameters, provides a scalable and relatively simple method to consistently produce high-bioavailability formulations compared to conventional mixing methods.
4Ease of manufacture
If current formulations are used, then manufacturing is straightforward, but release of cannabinoids is too low
Solution Approach 1:
The patent changes the physical state of cannabinoids to amorphous form, which has higher molecular mobility and lower activation energy for dissolution. This parameter change significantly accelerates the release rate of cannabinoids from the formulation, improving productivity and therapeutic onset while maintaining ease of manufacture through hot melt extrusion technology.
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 composition significantly increases the solubility and bioavailability of non-euphoric cannabinoids, ensuring they are homogeneously distributed and retained in a stable form, improving their therapeutic efficacy.
Implementation Method 1
hot melt extrusion to create a solid dispersion
Implementation Method 2
hot melt extrusion to create a solid dispersion
Data Source
AI summary
The present invention relates to a composition in the form of a friable/brittle thermoformed extrudate comprising at least one natural or synthetic non-euphoric cannabinoid and at least one natural or synthetic carrier chosen from the group consisting of amino acids, natural or synthetic peptides and polypeptides, natural or synthetic proteins, natural or synthetic saccharides, natural or synthetic lipids, urea, the derivatives thereof and the mixtures thereof.


