Cannabis tablets
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Cannabis Tablets: Enhancing Bioavailability and Therapeutic Potential
Introduction to Cannabis Tablets
Cannabis tablets, particularly those containing Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD), are gaining attention for their potential therapeutic benefits. However, the oral administration of these cannabinoids presents challenges due to their low bioavailability and significant first-pass metabolism1 2. Recent research has focused on optimizing formulations to improve the absorption and effectiveness of these compounds.
Self-Emulsifying Drug Delivery Systems (SEDDS)
Enhancing Bioavailability with SEDDS
One innovative approach to improve the bioavailability of cannabis extracts is the use of self-emulsifying drug delivery systems (SEDDS). These systems enhance the dissolution and absorption of cannabinoids by forming fine oil-in-water emulsions upon contact with gastrointestinal fluids1. However, liquid SEDDS formulations often suffer from stability issues.
Development of Solid SEDDS Tablets
To address stability concerns, researchers have developed solid SEDDS formulations. A study optimized directly compressible self-emulsifying tablets containing cannabis extract obtained from supercritical carbon dioxide extraction. The solidification process involved adsorbing the liquid SEDDS onto solid carriers like colloidal silicon dioxide and microcrystalline cellulose, followed by compression into tablets1. The optimized tablets demonstrated improved dissolution rates, particularly for Δ9-tetrahydrocannabinol, and were capable of emulsifying into small nano-sized droplets, enhancing bioavailability1.
Pharmacokinetics of Oral THC
Variability in Absorption
The pharmacokinetics (PK) of oral THC are highly variable, with delayed peak plasma concentrations compared to other administration routes. This variability is influenced by the formulation type, with capsules and tablets showing different absorption profiles2. A systematic review highlighted the need for further research to understand and mitigate this unpredictability to improve the effectiveness and safety of oral THC formulations2.
Promising Formulations: Namisol®
Namisol® is a novel THC tablet formulation designed to improve absorption and provide a rapid onset of therapeutic effects. Clinical studies have shown that Namisol® has a beneficial PK profile, with quicker Tmax and more consistent plasma concentrations compared to other oral THC formulations like dronabinol and nabilone3. This formulation has shown promising pharmacodynamic effects, including improved body sway, external perception, and alertness, making it a potential candidate for therapeutic use3.
Therapeutic Applications and Efficacy
Pain Management
Despite the potential benefits, the efficacy of THC tablets in pain management remains inconclusive. A phase 2 study investigating the analgesic effects of an oral THC tablet in patients with chronic abdominal pain found no significant difference in pain relief compared to a placebo4. This suggests that while THC tablets are well-absorbed and tolerated, their effectiveness in pain management may be limited or require further optimization.
Psychiatric Disorders
The application of medicinal cannabis in psychiatric disorders is an emerging field. Preliminary evidence suggests that cannabinoids, particularly CBD, may have potential benefits in reducing social anxiety and improving sleep and post-traumatic stress disorder symptoms7. However, the evidence is still nascent, and high-THC formulations should be used cautiously, especially in individuals with anxiety or psychotic disorders7.
Conclusion
Cannabis tablets, particularly those utilizing advanced delivery systems like SEDDS, show promise in enhancing the bioavailability and therapeutic potential of cannabinoids. While formulations like Namisol® demonstrate improved pharmacokinetics and rapid therapeutic effects, the efficacy of THC tablets in pain management and psychiatric disorders requires further investigation. Continued research and optimization are essential to fully realize the benefits of cannabis tablets in medical applications.
Sources and full results
Most relevant research papers on this topic
Fabrication and Optimization of Directly Compressible Self-Emulsifying Tablets Containing Cannabis Extract Obtained from Supercritical Carbon Dioxide Extraction
Directly compressible self-emulsifying tablets successfully enhanced the dissolution of cannabis extract, with 9-tetrahydrocannabinol showing higher dissolution than cannabidiol.
Oral Administration of Cannabis and Δ-9-tetrahydrocannabinol (THC) Preparations: A Systematic Review
Oral THC absorption is highly variable, with higher variability in baked goods and oil forms, highlighting the need for further investigations to enhance effectiveness and safety in medicinal use.
Systematic Review
Rigorous JournalNovel Δ(9) -tetrahydrocannabinol formulation Namisol® has beneficial pharmacokinetics and promising pharmacodynamic effects.
Oral Namisol® has a beneficial pharmacokinetic profile and quick onset of therapeutic effects, making it a promising treatment option for various indications.
RCTRigorous Journal
Highly CitedTetrahydrocannabinol Does Not Reduce Pain in Patients With Chronic Abdominal Pain in a Phase 2 Placebo‐controlled Study
THC tablets did not significantly reduce pain measures in patients with chronic abdominal pain, but were safe and well-tolerated during a 50-day to 52-day treatment period.
RCTHighly CitedEfficacy and safety of a fatty acid amide hydrolase inhibitor (PF-04457845) in the treatment of cannabis withdrawal and dependence in men: a double-blind, placebo-controlled, parallel group, phase 2a single-site randomised controlled trial.
PF-04457845 effectively reduces cannabis withdrawal symptoms and self-reported use in men with cannabis dependence, improving their quality of life.
RCTRigorous JournalHighly CitedCannabis, from plant to pill
Cannabis therapeutics can be effectively delivered through standardized growth and extraction, utilizing the plant's diverse cannabinoids and terpenes for therapeutic benefits.
Very Rigorous JournalHighly CitedMedicinal cannabis for psychiatric disorders: a clinically-focused systematic review
Medicinal cannabis shows encouraging evidence for treating various psychiatric disorders, but caution is needed due to potential safety concerns.
Systematic ReviewVery Rigorous JournalHighly CitedCannabis and Pain: A Clinical Review
Cannabis pharmacotherapy for pain shows modest evidence of effectiveness, but more research is needed to address potential side effects and risks.
Systematic ReviewHighly CitedPractical considerations in medical cannabis administration and dosing.
Cannabis medicine should be administered at low doses, preferably in conjunction with CBD, to avoid psychoactive effects and tolerance, while CBD may require higher doses for pain, inflammation, and anxiety relief.
Highly CitedCannabis, cannabinoids, and health
Cannabis use has harmful psychiatric and addictive effects, with synthetic cannabinoid use increasing, but certain cannabinoids and their synthetic derivatives have therapeutic properties for certain indications.
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