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

VSEngineering Contradiction Analysis

1Reliability

If non-euphoric cannabinoids are used in current formulations, then therapeutic effects are achieved, but solubility and bioavailability are too low

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidbioavailability
Core Design Contradiction:
ReliabilityVSQuantity of substance

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.

Inventive Principle:
Principle #35Parameter changes

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.

Inventive Principle:
Principle #40Composite materials

2Reliability

If non-euphoric cannabinoids are used in current formulations, then therapeutic effects are achieved, but dispersion in aqueous phase is insufficient

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoiddispersion stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

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.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Ease of manufacture

If conventional formulation methods are used, then manufacturing is simple, but solubility and bioavailability are inadequate

Engineering Contradiction:
Improveformulation simplicityVSAvoidbioavailability
Core Design Contradiction:
Ease of manufactureVSQuantity of substance

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.

Inventive Principle:
Principle #35Parameter changes

4Ease of manufacture

If current formulations are used, then manufacturing is straightforward, but release of cannabinoids is too low

Engineering Contradiction:
Improveformulation simplicityVSAvoidcompound release rate
Core Design Contradiction:
Ease of manufactureVSProductivity

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.

Inventive Principle:
Principle #35Parameter changes

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

Methodology Applied
Scientific EffectMelting: Melting

Implementation Method 2

hot melt extrusion to create a solid dispersion

Methodology Applied
Scientific EffectExtrusion: Extrusion

Data Source

PatentUS20220273585A1Composition comprising at least one natural or synthetic non-euphoric cannabinoid and its method of manufacture
Publication Date: 2022.09.01 ELEONOR SPRL
  • US20220273585A1 patent drawing
  • US20220273585A1 patent drawing
  • US20220273585A1 patent drawing

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.