Cannabinoid Granulate with Sucrose Mono-Ester Binding for Bioavailability
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Solution Overview
Problem
Peroral administration of cannabinoids results in poor bioavailability due to the first pass effect, where substances are rapidly metabolized in the liver, and hydrophobic cannabinoids are poorly absorbed from the intestinal environment due to low solubility and dispersibility in water.
Innovation Solution
A granulate comprising lactose particles held together by a binding component containing at least 80 wt.% sucrose mono-ester of C8-C18 fatty acids, which enhances the solubility and absorption of cannabinoids across the intestines, allowing for effective peroral delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If peroral administration of cannabinoids is used, then convenience of administration is improved, but bioavailability deteriorates due to first pass effect
Solution Approach 1:
The patent changes the physical and chemical parameters of the cannabinoid formulation by incorporating it into a lipophilic matrix with surfactants and co-solvents, creating a nanosuspension or micellar system that alters solubility and absorption characteristics to overcome first pass metabolism
Solution Approach 2:
The invention uses composite material systems combining cannabinoids with lipophilic matrices, surfactants, and co-solvents to create a formulation that enhances bioavailability while maintaining peroral administration convenience
2Ease of manufacture
If hydrophobic cannabinoids are administered perorally, then ease of formulation is improved, but absorption from intestinal environment deteriorates due to poor solubility and dispersibility in water
Solution Approach 1:
The patent introduces surfactants and co-solvents as intermediary substances that mediate between the hydrophobic cannabinoid and the hydrophilic intestinal environment, enabling solubilization and enhancing absorption without complicating the formulation process
Solution Approach 2:
The invention changes the solubility parameters of cannabinoids by forming nanosuspensions or micellar systems that increase surface area and dispersibility in aqueous environments while maintaining ease of formulation
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 granulate formulation achieves sufficient bioavailability of cannabinoids despite the first pass effect, with rapid dissolution and absorption of the cannabinoid into the bloodstream, improving the efficacy of peroral administration.
Implementation Method 1
a binding component comprising a cannabinoid and a sucrose fatty acid mono-ester... enhances the solubility and absorption of cannabinoids
Implementation Method 2
absorption of the cannabinoid into the bloodstream
Data Source
AI summary
The present invention relates to a granulate comprising granules made up of 40-99 wt. % of lactose particles and 1-60 wt. % of a binding component that holds together the lactose particles within the granules. Said granules have a mass weighted average diameter of 50-500 μm and said binding component is a solid dispersion or a solid solution of 10-75 wt. % of a cannabinoid in 25-80 wt. % of a lipophilic matrix. The lipophilic matrix contains at least 80 wt. % sucrose fatty acid mono-ester, the fatty acid residue being selected from C8-C18 fatty acids.The aforementioned granulate can be processed into oral dosage units in the form of tablets for oral delivery.The invention further provides a method for the manufacture of the granulate.