CBD Eutectic Mixtures for High Drug Loading
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Cannabidiol (CBD) has low solubility and bioavailability in existing pharmaceutical formulations, making it difficult to achieve high drug loading and effective absorption, particularly due to its low binding constant with endocannabinoid receptors, which requires high doses and complicates incorporation into solid dosage forms.
Innovation Solution
A eutectic mixture comprising CBD and physiologically acceptable organic compounds, such as fatty alcohols, cyclic alcohols, and glycerides, is formed to increase solubility and bioavailability, with melting points lower than CBD, allowing for enhanced drug loading and absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If CBD is incorporated into solid dosage forms to achieve high drug loading, then the required dose can be delivered, but the low solubility and bioavailability of CBD prevent effective absorption
Solution Approach 1:
The patent changes the physical-chemical parameters of CBD by forming eutectic mixtures with compounds like menthol, thymol, and terpenes. This phase transition approach transforms solid CBD into a liquid eutectic state at lower temperatures, fundamentally altering its solubility characteristics and enabling high drug loading while maintaining bioavailability through improved dissolution properties
Solution Approach 2:
The invention creates composite eutectic mixture formulations combining CBD with physiologically acceptable compounds such as menthol, thymol, and various terpenes. These composite materials exhibit synergistic properties where the mixture demonstrates enhanced solubility and bioavailability compared to pure CBD, resolving the contradiction between drug loading quantity and absorption reliability
2Quantity of substance
If the binding constant of CBD with endocannabinoid receptors is low, then higher doses are required to achieve biological activity, but high doses complicate incorporation into solid dosage forms due to CBD's low solubility
Solution Approach 1:
The patent utilizes phase transition by forming liquid eutectic mixtures at temperatures below the melting point of pure CBD. This phase change from solid to liquid state enables the incorporation of high doses of CBD into dosage forms, as the liquid eutectic can be more easily formulated into capsules, tablets, or other solid dosage forms while maintaining the required high drug content
Solution Approach 2:
The eutectic forming compounds (menthol, thymol, terpenes) act as intermediary substances that facilitate the incorporation of high doses of CBD into dosage forms. These intermediaries create a soluble complex with CBD, enabling high drug loading while maintaining manufacturability through improved physical properties of the mixture
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 eutectic mixtures significantly improve CBD solubility and bioavailability, enabling the development of high-loading pharmaceutical formulations with increased transdermal penetration and anti-inflammatory activity, and improved stability during storage.
Implementation Method 1
Eutectic mixture (EM) is defined as a homogeneous mixture of two or more components that melts or solidifies at a single temperature that is lower than the melting point of any of the individual constituents
Data Source
AI summary
Pharmaceutical compositions comprising eutectic mixtures comprising Cannabidiol (CBD) and at least one physiologically acceptable organic compound, allowing to increase solubility of cannabinoid in pharmaceutical compositions and to improve drug loading, drug absorption and bioavailability of CBD after administration. Methods of increasing cannabidiol (CBD) solubility for use in pharmaceutical formulations with high CBD loading