Enteric Coated Multiparticulate Cannabinoid Dosage for GI Targeting
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
There is a shortage of oral cannabinoid dosage forms that can specifically target areas of inflammation in the gastrointestinal tract and bypass CB2 receptors in the stomach, limiting effective treatment for gastrointestinal disorders.
Innovation Solution
An oral pharmaceutical dosage form comprising a solid matrix of microcrystalline cellulose and cannabinoid oil, designed as spheroidal particulates with an enteric coating to release the cannabinoid oil in specific sections of the gastrointestinal tract, such as the duodenum, jejunum, or ileum, to target inflammation effectively.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If conventional oral cannabinoid dosage forms are used, then cannabinoids can be administered orally, but they cannot specifically target areas of inflammation in the gastrointestinal tract and cannot bypass CB2 receptors in the stomach
Solution Approach 1:
The dosage form is segmented into multiple particles with different sizes (ranging from 0.5mm to 3mm) that can be distributed throughout the gastrointestinal tract. Each particle acts as an independent unit that can reach different anatomical locations, enabling targeted delivery to specific inflamed areas such as the duodenum, jejunum, or ileum while bypassing stomach CB2 receptors.
Solution Approach 2:
The invention applies local quality by creating particles with specific size ranges that correspond to different release locations in the GI tract. Smaller particles (0.5-1.7mm) target the duodenum, medium particles (0.5-1.7mm) target the jejunum, and larger particles (1.8-3mm) provide sustained release throughout the intestines. This localized approach allows cannabinoids to be delivered precisely where inflammation occurs rather than uniformly throughout the system.
2Speed
If cannabinoids are released in the stomach, then they can be quickly absorbed, but they activate CB2 receptors in the stomach causing unwanted side effects
Solution Approach 1:
The invention extracts the harmful interaction between cannabinoids and stomach CB2 receptors by designing particles that bypass the stomach entirely. The enteric coating and specific particle size distribution ensure that cannabinoids are not released in the stomach, thereby eliminating activation of gastric CB2 receptors and associated side effects while still achieving rapid absorption in the small intestine where inflammation typically occurs.
Solution Approach 2:
The enteric coating acts as an intermediary barrier that prevents cannabinoid release in the stomach. This coating layer protects the cannabinoids from interacting with stomach CB2 receptors and allows them to pass through the stomach intact, releasing only in the more alkaline environment of the small intestine where therapeutic effect is needed without harmful side effects.
3Area of stationary object
If cannabinoids are released throughout the entire gastrointestinal tract, then broad coverage is achieved, but sustained release for at least 6 hours cannot be maintained
Solution Approach 1:
The dosage form is divided into particles of different sizes that release cannabinoids at different rates and locations. Larger particles (1.8-3mm) provide sustained release throughout the intestines for at least 6 hours, while smaller particles (0.5-1.7mm) provide more rapid release in specific sections. This segmentation allows the system to simultaneously achieve broad coverage and sustained release by distributing different particle types throughout the GI tract.
Solution Approach 2:
The invention implements periodic action through the staggered release of cannabinoids from particles of different sizes as they traverse the gastrointestinal tract. Larger particles continue releasing cannabinoids over extended periods (at least 6 hours) as they move through the intestines, while smaller particles release their content more rapidly at specific locations. This creates a periodic, sustained therapeutic effect throughout the treatment period.
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
This formulation allows for targeted and sustained release of cannabinoid oil in the gastrointestinal tract, effectively treating gastrointestinal disorders by minimizing side effects and ensuring the cannabinoid oil reaches the site of inflammation, providing relief from symptoms like IBS, Crohn's disease, and ulcerative colitis.
Implementation Method 1
The individual particulates have a solid core including an effective amount of cannabinoid oil bound in microcrystalline cellulose and an enteric coating over the solid core
Implementation Method 2
The cannabinoid oil bound in microcrystalline cellulose may be substantially dry
Data Source
AI summary
Cannabinoid oil compositions may be used to treat gastrointestinal disorders. An example of the composition is an oral multiparticulate dosage form including a plurality of individual particulates including a solid core with an effective amount of cannabinoid oil bound in microcrystalline cellulose therein and an enteric coating over the solid core.