Self-Emulsifying Cannabinoid Tablets for Stable GI Uptake
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Solution Overview
Problem
Existing carrier systems for gastrointestinal delivery of cannabinoids face challenges such as degradation, low uptake, steric hindrance, unsuitable mouthfeel, and inadequate sensorics properties, particularly when high doses are administered, leading to inefficient delivery and adverse effects.
Innovation Solution
Development of orally dissolvable or chewable tableted powder formulations containing self-emulsifying systems with surfactants, lipids, and cannabinoids, stabilized by polyethylene glycol moieties, which are stable at pH 1-4 and facilitate gastrointestinal delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If powder formulations are used for gastrointestinal delivery of cannabinoids, then the capability to withstand low pH in the stomach is improved, but the uptake in the gastrointestinal tract is reduced due to degradation
Solution Approach 1:
The system divides the cannabinoid delivery into separate functional components: a stable powder carrier that withstands stomach acid, and a self-emulsifying system that activates in the intestine to release cannabinoids. This segmentation allows the formulation to survive gastric conditions while ensuring subsequent intestinal uptake.
Solution Approach 2:
The powder formulation is pre-designed to resist gastric acid degradation before reaching the intestine. The self-emulsifying system is pre-positioned within the powder matrix, ready to activate upon contact with intestinal fluids, ensuring immediate emulsification and uptake without prior degradation.
2Quantity of substance
If carrier systems are used to deliver high loads of cannabinoids, then the dosage capacity is improved, but the mouthfeel becomes unsuitable with sandy feeling and creaking sound
Solution Approach 1:
The system uses a composite formulation combining multiple excipients (microcrystalline cellulose, mannitol, sucrose, stearic acid) with the self-emulsifying cannabinoid system. This composite approach allows high cannabinoid loading while the excipients provide a smooth, pleasant mouthfeel that masks the texture of the carrier particles.
Solution Approach 2:
Different components of the powder formulation serve localized functions: some particles provide structural stability, others provide smooth texture, and the self-emulsifying system provides the active cannabinoid delivery. This local differentiation of functions allows high loading without compromising overall mouthfeel.
3Ease of operation
If the carrier system is released in the oral cavity, then the convenience of oral administration is improved, but the delivery efficiency to gastrointestinal tract is reduced
Solution Approach 1:
The self-emulsifying system acts as an intermediary between the oral cavity and gastrointestinal tract. Upon release in the mouth, it remains stable during swallowing and then activates in the intestine to form emulsions that enhance absorption. This intermediary behavior allows convenient oral administration while ensuring efficient intestinal delivery.
Solution Approach 2:
The system transitions from a stable powder state during oral administration to an active emulsifying state in the intestine. This dynamic transformation allows the formulation to remain inert and convenient during swallowing, then become highly active for absorption when it reaches the target site.
4Productivity
If surfactants with polyethylene glycol moiety are used in self-emulsifying systems, then the gastrointestinal uptake is improved, but the steric hindrance increases
Solution Approach 1:
The system optimizes the molecular weight and chain length of the polyethylene glycol moiety in the surfactant to achieve the right balance. By carefully controlling these parameters, the formulation achieves sufficient steric protection to enhance intestinal uptake while minimizing excessive hindrance that would block 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 formulations provide high load and stable delivery of cannabinoids, improving uptake in the gastrointestinal tract, reducing adverse effects, and enhancing sensorics properties like texture and flavor perception.
Implementation Method 1
self-emulsifying systems comprising surfactants, lipids, and cannabinoids, with optional waxes and water-soluble agents, designed to withstand low pH and facilitate gastrointestinal delivery
Implementation Method 2
the one or more self-emulsifying systems includes i) at least one or more surfactants, one or more lipids and one or more isolated or synthetic cannabinoids
Data Source
AI summary
An orally dissolvable or chewable tableted powder formulation is presented. The formulation includes one or more carrier systems including one or more liquid or solid self-emulsifying systems loaded with cannabinoids in an amount of at least 10% by weight of the tableted powder formulation. The one or more self-emulsifying systems includes: at least one or more surfactants, one or more lipids and one or more isolated or synthetic cannabinoids when self-emulsifying system is a liquid self-emulsifying system, and at least one or more surfactants, one or more waxes and one or more isolated or synthetic cannabinoids when self-emulsifying system is a solid self-emulsifying system. The formulation further includes one or more water-soluble agents in an amount of 20-80% by weight of the tableted powder formulation and one or more flavors. The one or more surfactants includes one or more surfactants having a chemical structure that includes a polyethylene glycol moiety.