Porous Sorbent Cannabinoid Formulation for Oral Bioavailability
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Solution Overview
Problem
Cannabinoids exhibit low bioavailability and susceptibility to degradation due to poor solubility and susceptibility to the first pass effect when administered orally, leading to inefficient absorption and distribution in the body.
Innovation Solution
A pharmaceutical formulation comprising a particulate porous sorbent coated with a nonionic surfactant and cannabinoids, designed for delayed release in the small intestine, enhancing solubility and stability in the gastrointestinal tract.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If cannabinoids are administered orally in traditional formulations, then they can be easily taken and distributed, but their bioavailability is low due to poor solubility and first pass metabolism
Solution Approach 1:
The patent uses a nonionic surfactant as an intermediary substance to enhance the solubility and stability of lipophilic cannabinoids in the aqueous gastrointestinal environment. The surfactant forms micelles that encapsulate the hydrophobic cannabinoid molecules, enabling them to survive stomach acid and first-pass metabolism while maintaining solubility throughout the digestive tract.
Solution Approach 2:
The formulation creates a composite system combining lipophilic cannabinoids with hydrophilic surfactant molecules. This composite structure allows the hydrophobic active ingredient to be delivered through the hydrophilic gastrointestinal tract, resolving the solubility contradiction while maintaining ease of oral administration.
2Reliability
If cannabinoids are formulated to increase solubility in water, then bioavailability may improve, but they become susceptible to degradation from light, oxygen, and acidic pH
Solution Approach 1:
The patent applies beforehand cushioning by formulating cannabinoids with stabilizing excipients including antioxidants and pH buffers that protect the compound from degradation before it reaches the intestine. The surfactant micelles provide a protective microenvironment that shields cannabinoids from light, oxygen, and acidic conditions during gastrointestinal transit.
Solution Approach 2:
The surfactant micelle structure creates an inert protective environment around the cannabinoid molecules, isolating them from harmful environmental factors such as light, atmospheric oxygen, and acidic pH conditions in the stomach, thereby maintaining chemical stability while enabling solubility.
3Manufacturing precision
If cannabinoids are administered as solid formulations, then dosing is consistent, but absorption is poor due to poor dispersibility in water
Solution Approach 1:
The patent changes the physical-chemical parameters of the cannabinoid formulation by incorporating surfactants that alter the surface properties and solubility characteristics. This transforms the solid formulation into a colloidal suspension with improved dispersibility while maintaining precise dosing through controlled manufacturing of the semi-solid formulation.
Solution Approach 2:
The formulation utilizes phase transition concepts by creating a semi-solid or viscous formulation that maintains structural integrity for precise dosing but transitions to a dispersed colloidal state upon contact with gastrointestinal fluids, enabling both dosing consistency and improved absorption.
4Speed
If cannabinoids are released immediately in the stomach, then absorption could occur quickly, but they are metabolized by the first pass effect in the liver
Solution Approach 1:
The patent applies preliminary action by designing a formulation that protects cannabinoids during stomach transit and enables them to reach the intestine in an intact, active state. The surfactant micelles and protective excipients prepare the cannabinoids for delayed release in the intestine, bypassing first-pass metabolism while maintaining readiness for rapid absorption when released.
Solution Approach 2:
The formulation enables cannabinoids to skip the harmful first-pass metabolism by rushing through the stomach and small intestine in a protected, solubilized state within surfactant micelles, allowing direct absorption into the bloodstream before liver metabolism can occur, thereby increasing systemic availability.
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 formulation significantly improves the bioavailability and dispersibility of cannabinoids, achieving 40-60% release in the gastrointestinal tract, overcoming the first pass effect and enhancing absorption.
Implementation Method 1
a nonionic surfactant is applied to the particulate porous sorbent
Implementation Method 2
a particulate porous sorbent onto which is applied a mixture of at least one cannabinoid with a nonionic surfactant
Data Source
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AI summary
The invention provides a pharmaceutical formulation containing a particulate porous sorbent selected from the group comprising aluminosilicates and their salts, with a neutral or basic pH and with a particle size in the range of 50 to 800 µm, on which a mixture of polyoxyethylene sorbitan monooleate (Polysorbate 80) with at least one cannabinoid selected from cannabidiol, cannabigerol, cannabinol, D9-THC and D8-THC is applied. The formulation improves bioavailability and release profile of the cannabinoids.