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Novel Δ(9) -tetrahydrocannabinol formulation Namisol® has beneficial pharmacokinetics and promising pharmacodynamic effects.

Linda E. Klumpers, Tim L Beumer, Johan G C Van Hasselt, Astrid Lipplaa, Lennard B Karger, H Daniël Kleinloog, Jan I Freijer, Marieke L De Kam, Joop van Gerven

British Journal of Clinical Pharmacology July 2012 DOI: 10.1111/j.1365-2125.2012.04164.x (opens in new tab)

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Study at a glance

AI-extracted from the abstract
Characteristics Randomized, double-blind, double-dummy, crossover, first-in-human pharmacokinetic and pharmacodynamic study Peer reviewed
Sample size 21
Population Healthy male and female volunteers
Intervention placebo
Dose 5 mg THC sublingual and oral; 6.5 mg and 8.0 mg oral THC
Measures body sway, visual analogue scales (VAS) for mood, psychedelic effects and alertness, heart rate, THC and 11-OH-THC plasma concentrations
Topics Cannabis
Key points Oral Namisol produced quicker and less variable THC plasma concentrations than sublingual administration, with apparent half-life 72-80 minutes, time to peak 39-56 minutes, and peak concentration 2.92-4.69 ng/ml. THC caused measurable pharmacodynamic effects including increased body sway (60.8%), altered perception and mood, and a 5.6 beats per minute rise in heart rate. The authors conclude that oral Namisol has promising pharmacokinetic and pharmacodynamic characteristics and was well tolerated, but call for studies in patients.

Abstract

• Cannabis based medicines are registered as a treatment for various indications, such as pain and spasms in multiple sclerosis (MS) patients, and anorexia and nausea in patients with HIV or receiving cancer treatment. • the pharmacokinetics of the various administration routes of cannabis and cannabis based medicines are variable and dosing is hard to regulate. • Namisol is a new tablet containing pure THC (>98%) that has a beneficial pharmacokinetic profile after oral administration. • Namisol gives a quick onset of pharmacodynamic effects in healthy volunteers, which implies a rapid initiation of therapeutic effects in patients. Among the main disadvantages of currently available Δ(9) -tetrahydrocannabinol (THC) formulations are dosing difficulties due to poor pharmacokinetic characteristics. Namisol® is a novel THC formulation, designed to improve THC absorption. The study objectives were to investigate the optimal administration route, pharmacokinetics (PK), pharmacodynamics (PD) and tolerability of Namisol®. This first in human study consisted of two parts. Panel I included healthy males and females (n = 6/6) in a double-blind, double-dummy, randomized, crossover study with sublingual (crushed tablet) and oral administration of Namisol® (5 mg THC). Based on these results, male and female (n = 4/5) participants from panel I received oral THC 6.5 and 8.0 mg or matching placebo in a randomized, crossover, rising dose study during panel II. PD measurements were body sway; visual analogue scales (VAS) mood, psychedelic and heart rate. THC and 11-OH-THC population PK analysis was performed. Sublingual administration showed a flat concentration profile compared with oral administration. Oral THC apparent t(1/2) was 72-80 min, t(max) was 39-56 min and C(max) 2.92-4.69 ng ml(-1) . THC affected body sway (60.8%, 95% CI 29.5, 99.8), external perception (0.078 log mm, 95% CI 0.019, 0.137), alertness (-2.7 mm, 95% CI -4.5, -0.9) feeling high (0.256 log mm, 95% CI 0.093, 0.418) and heart rate (5.6 beats min(-1) , 95% CI 2.7, 6.5). Namisol® was well tolerated. Oral Namisol® showed promising PK and PD characteristics. Variability and t(max) of THC plasma concentrations were smaller for Namisol® than reported for studies using oral dronabinol and nabilone. This study was performed in a limited number of healthy volunteers. Therefore, future research on Namisol® should study clinical effects in patient populations.

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Cannabidiol (CBD) content in vaporized cannabis does not prevent tetrahydrocannabinol (THC)-induced impairment of driving and cognition Healthy volunteers with a history of light cannabis use 2019 Randomized, double-blind, within-subjects crossover n = 14

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