Cannabinoid SNEDDS Tablet Composition for Rapid Gastric Dissolution
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Solution Overview
Problem
Oral formulations of cannabinoids like CBD and THC suffer from poor solubility and bioavailability due to their lipophilic and highly hydrophobic nature, necessitating improved pharmaceutical compositions for effective oral administration.
Innovation Solution
A compressed tablet formulation with an intragranular portion containing a self-nanoemulsifying drug delivery system (SNEDDS) adsorbed on a porous solid carrier, comprising cannabinoids, solubilizing agents, and emulsifying agents, and an extragranular portion with porous solid carriers, disintegrants, diluents, and lubricants, designed to enhance solubility and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral formulations of cannabinoids are used, then patient compliance is improved, but solubility and bioavailability deteriorate due to lipophilic nature
Solution Approach 1:
The patent employs a composite self-nanoemulsifying drug delivery system (SNEDDS) comprising multiple components: solubilizing agents (e.g., PEG 400, PEG 3350), emulsifying agents (e.g., polysorbate 80, lecithin), and carrier oils (e.g., medium-chain triglycerides). This composite formulation creates a synergistic effect that enables hydrophobic cannabinoids to form stable nanoemulsions in aqueous gastric fluid, resolving the contradiction between oral administrability and solubility.
Solution Approach 2:
The invention changes the physical state and surface properties of the cannabinoid formulation by converting it into a self-nanoemulsifying system. The SNEDDS formulation undergoes phase transformation upon contact with gastric fluid, forming nanoscale emulsion droplets that dramatically increase surface area and improve dissolution rate, thereby enhancing bioavailability while maintaining oral dosage form advantages.
2Productivity
If SNEDDS is adsorbed on porous solid carrier, then dissolution rate is improved, but formulation complexity increases
Solution Approach 1:
The patent utilizes porous solid carriers (e.g., porous silicon dioxide, porous calcium phosphate) with high surface area and controlled pore structures to adsorb the SNEDDS formulation. The porous structure provides extensive adsorption sites that hold the nanoemulsifying system, enabling rapid release and dissolution upon contact with gastric fluid. This approach accelerates dissolution rate while the porous material's inherent properties simplify the overall formulation design.
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 ensures rapid dissolution of cannabinoids in gastric fluid, achieving at least 70% dissolution within 30 minutes, maintaining solubility in an oil phase, and providing a stable, effective oral dosage form.
Implementation Method 1
a self-nanoemulsifying drug delivery system (SNEDDS) adsorbed on the carrier, wherein the SNEDDS comprises: at least one cannabinoid; one or more solubilizing agents; one or more emulsifying agents; and one or more carrier oils
Implementation Method 2
one or more emulsifying agents selected from physiologically acceptable nonionic surfactants
Implementation Method 3
a first porous solid carrier comprising a physiologically acceptable salt that is soluble in gastric fluid or in an acidic aqueous media; a self-nanoemulsifying drug delivery system (SNEDDS) adsorbed on the carrier
Data Source
AI summary
A pharmaceutical composition in the form of a compressed tablet for oral administration. The composition has an intragranular portion including a first porous solid carrier with a physiologically acceptable salt that is soluble in gastric fluid/an acidic aqueous media, and a self-nanoemulsifying drug delivery system (SNEDDS) adsorbed on the carrier. The SNEDDS includes: at least one cannabinoid; one or more solubilizing agents selected from physiologically acceptable organic compounds including: alcohols C8-C18, cyclic alcohols, aromatic alcohols, glycerides, polyethylene glycols, polyethylene glycol esters, aromatic esters, phenols, tocopherols, phospholipids, polyoxylglycerides, or polyoxyethylene stearates; one or more emulsifying agents selected from physiologically acceptable nonionic surfactants; and one or more carrier oils. The composition has an extragranular portion including: an optional second porous solid carrier including a physiologically acceptable salt that is soluble in gastric fluid/an acidic aqueous media; one or more disintegrants; one or more diluents; and one or more lubricants.