Cannabinoid Formulation Bioavailability via Poloxamer SEDDS
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Solution Overview
Problem
Cannabinoids, such as CBD, face challenges with low bioavailability and stability due to their lipophilic nature and susceptibility to first-pass liver metabolism when taken orally, and existing self-emulsifying drug delivery systems often have reduced effectiveness due to lipid-based surfactant interactions with gastric fluids.
Innovation Solution
A novel oral pharmaceutical formulation classified as Type IV or Type IV-like, comprising a cannabinoid, poloxamer, and a solvent, with no oil, enhancing bioavailability and stability by using a solvent defined by specific chemical structures and poloxamers like poloxamer 124 and 188, which improves absorption and storage stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If lipophilic cannabinoids are administered orally, then they can be delivered systemically, but their bioavailability is low due to poor water solubility and first-pass liver metabolism
Solution Approach 1:
The patent changes the physical-chemical parameters of the cannabinoid formulation by converting it from a pure lipophilic substance to a self-emulsifying system containing surfactants and co-solvents. This creates micellar structures that alter the dissolution and absorption characteristics, enabling better aqueous dispersion and reduced first-pass metabolism while maintaining systemic delivery
Solution Approach 2:
The patent creates a composite formulation system combining the lipophilic cannabinoid with hydrophilic surfactants and co-solvents. This composite self-emulsifying drug delivery system (SEDDS) integrates both lipophilic and hydrophilic components to overcome the inherent solubility limitations and metabolic susceptibility of pure cannabinoids
2Reliability
If lipid-based surfactants are used in SEDDS formulations, then cannabinoid solubility is improved, but interaction with gastric lipases reduces emulsification capability and bioavailability
Solution Approach 1:
The patent applies local quality by selecting surfactants with specific hydrophilic-lipophilic balance (HLB) values and molecular structures that are resistant to lipase degradation in the gastric environment. The formulation uses non-ionic surfactants and specific co-solvent combinations that maintain emulsification capability despite the presence of gastric lipases
Solution Approach 2:
The patent introduces co-solvents and protective excipients that act as intermediaries between the lipid-based surfactants and gastric lipases. These intermediary substances reduce the direct interaction between lipases and surfactants, preserving the emulsification capability of the SEDDS formulation
3Reliability
If CBD is administered orally, then it can be delivered to the body, but its instability leads to unpredictable bioavailability
Solution Approach 1:
The patent applies beforehand cushioning by incorporating antioxidants and stabilizing excipients in the SEDDS formulation that protect CBD from degradation before it reaches the absorption site. These protective agents prevent oxidative degradation and hydrolysis during storage and gastrointestinal transit, ensuring predictable bioavailability
Solution Approach 2:
The patent creates a composite formulation system that integrates CBD with protective excipients, surfactants, and co-solvents in a stable matrix. This composite structure protects the unstable cannabinoid from environmental factors while maintaining its therapeutic activity and predictable absorption
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 enhances cannabinoid bioavailability and stability, allowing for reduced dosage and extended shelf life, with improved rehydration and release properties, and is effective in treating various conditions including epilepsy and autism spectrum disorders.
Implementation Method 1
Self Emulsifying Drug Delivery Systems (SEDDS) have been used to offer improved administration of cannabinoids
Implementation Method 2
CBD is soluble in ethanol (36 mg/mL) and dimethylsulfoxide DMSO (60 mg/mL)
Implementation Method 3
Bioavailability of pharmaceutical substances taken perorally, first of all, depends on the extent to which the pharmaceutically active substance is absorbed from the intestinal environment across the intestinal mucosa
Data Source
AI summary
The present invention relates to an oral pharmaceutical formulation comprising a cannabinoid. The formulation may take the form of a mucoadhesive gel, a tablet, a powder, a liquid gel capsule, an oral solution, granules, extrudates or injectable.