Oil-Free Cannabinoid Oral Composition for Bioavailability
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Solution Overview
Problem
Cannabinoids, such as CBD, face challenges with poor bioavailability, instability, and rapid metabolism when administered orally due to their lipophilic nature and susceptibility to first-pass liver metabolism.
Innovation Solution
A novel oral pharmaceutical composition based on a Type IV or Type IV-like formulation, classified using the Lipid Formulation Classification System, which includes a core comprising a cannabinoid (cannabidiol) and a shell comprising a modified-release agent. The formulation is oil-free, containing cannabidiol in the range of 10 to 50 wt%, a solvent such as triethyl citrate, and a poloxamer like poloxamer 124 or 188, enhancing bioavailability and 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 poor due to poor solubility and first-pass metabolism
Solution Approach 1:
The patent uses a self-emulsifying drug delivery system (SEDDS) comprising oil, water-soluble surfactants, and co-solvents as an intermediary medium. This system facilitates the dissolution and absorption of lipophilic cannabinoids by forming microemulsions in the gastrointestinal tract, thereby improving bioavailability while protecting against first-pass metabolism through controlled release
Solution Approach 2:
The patent modifies the physical and chemical parameters of the cannabinoid delivery system by adjusting the composition ratios of oil (40-80 wt%), water-soluble surfactants (20-60 wt%), and co-solvents (0-50 wt%). These parameter changes optimize the formulation to achieve better solubility, stability, and absorption characteristics, directly addressing the poor bioavailability issue
2Stability of the object's composition
If lipid-based surfactants are used in SEDDS formulations, then emulsification is enhanced, but interaction with lipases reduces emulsification capability and bioavailability
Solution Approach 1:
The patent specifically changes the chemical nature of the surfactants from lipid-based to water-soluble surfactants (such as polysorbates, polyoxamers, and lecithin). This parameter change eliminates the problematic interaction with lipases while maintaining effective emulsification capability, thereby preserving bioavailability
Solution Approach 2:
The patent employs co-solvents (such as ethanol, propylene glycol, or polyethylene glycol) that are readily biodegradable and metabolized. These short-living components assist in the initial emulsification process but do not persist to cause long-term interference with digestive enzymes, thus avoiding the lipase interaction problem
3Productivity
If cannabinoids are released in the stomach, then absorption can begin, but harsh acidic conditions and enzymatic degradation reduce API stability
Solution Approach 1:
The patent incorporates pH-sensitive polymers and enteric coating materials in the SEDDS formulation that pre-condition the system to remain stable in acidic stomach environment. These materials prevent premature release and degradation of cannabinoids, ensuring they reach the more favorable intestinal environment for absorption while maintaining API stability
Solution Approach 2:
The self-emulsifying system acts as a protective intermediary that shields cannabinoids from direct exposure to harsh gastric conditions. The formulation's specific composition of surfactants and co-solvents creates a protective microenvironment that prevents enzymatic degradation while facilitating controlled release in the intestine where absorption is more efficient
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 enhances the bioavailability of cannabinoids, protects the API from harsh stomach conditions, and exhibits excellent stability under various storage conditions, allowing for targeted release in the gastrointestinal tract.
Implementation Method 1
the pharmaceutical formulation comprises a water soluble surfactant
Implementation Method 2
SEDDS (self-emulsifying drug delivery systems) generally consist of hard or soft capsules filled with a liquid or a gel that consists of lipophilic active pharmaceutical ingredient (API), oil (to dissolve the API) and a surfactant. Upon contact with gastric fluid, the SEDDS spontaneously emulsify due to the presence of surfactants.
Implementation Method 3
The oral pharmaceutical composition comprises a pharmaceutical formulation and at least one modified-release agent
Data Source
Figure 1
AI summary
The present invention relates to a novel cannabinoid oral pharmaceutical dosage form, or pharmaceutical composition, comprising a pharmaceutical formulation based on a Type IV or Type IV-like formulation, as classified using the Lipid Formulation Classification System. The oral pharmaceutical composition comprises a pharmaceutical formulation and at least one modified-release agent. By Type IV-like, it is meant that the pharmaceutical formulation comprises no oil, for example no triglycerides or mixed glycerides.