Metabolism of cannabidiol by the rat

Samara, Emil; Bialer, Meir; Harvey, David J.

doi:10.1007/bf03189976

Cited by 14 publications

(18 citation statements)

References 15 publications

(24 reference statements)

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“…Even though the metabolism of CBD was studied in several animal species (e.g., dogs and rats) [ 82 , 83 , 84 , 85 ] before, Harvey and Mechoulam were the first to report on the human CBD metabolism in the early 1990s [ 69 , 70 ]. As they measured human urine samples with a GC/MS method after the patients were orally administrated with CBD, they found over 30 metabolites, which were mainly hydroxylated in various positions.…”

Section: Resultsmentioning

confidence: 99%

Conversion of Cannabidiol (CBD) into Psychotropic Cannabinoids Including Tetrahydrocannabinol (THC): A Controversy in the Scientific Literature

Golombek

Müller

Barthlott

et al. 2020

Toxics

101

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Cannabidiol (CBD) is a naturally occurring, non-psychotropic cannabinoid of the hemp plant Cannabis sativa L. and has been known to induce several physiological and pharmacological effects. While CBD is approved as a medicinal product subject to prescription, it is also widely sold over the counter (OTC) in the form of food supplements, cosmetics and electronic cigarette liquids. However, regulatory difficulties arise from its origin being a narcotic plant or its status as an unapproved novel food ingredient. Regarding the consumer safety of these OTC products, the question whether or not CBD might be degraded into psychotropic cannabinoids, most prominently tetrahydrocannabinol (THC), under in vivo conditions initiated an ongoing scientific debate. This feature review aims to summarize the current knowledge of CBD degradation processes, specifically the results of in vitro and in vivo studies. Additionally, the literature on psychotropic effects of cannabinoids was carefully studied with a focus on the degradants and metabolites of CBD, but data were found to be sparse. While the literature is contradictory, most studies suggest that CBD is not converted to psychotropic THC under in vivo conditions. Nevertheless, it is certain that CBD degrades to psychotropic products in acidic environments. Hence, the storage stability of commercial formulations requires more attention in the future.

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Section: Resultsmentioning

confidence: 99%

Conversion of Cannabidiol (CBD) into Psychotropic Cannabinoids Including Tetrahydrocannabinol (THC): A Controversy in the Scientific Literature

Golombek

Müller

Barthlott

et al. 2020

Toxics

101

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“…Several studies showed that the metabolism of CBD in rats was different from that in humans [36, 42, 43], suggesting that the human-rat difference in the absolute bioavailability (i.e., very low in humans but moderate in rats) may be due to the lower first-pass metabolism of CBD in rats. Considering a future clinical study, where the present CBD-NE formulation is orally administered and its pharmacokinetic profile is compared with a conventional oil solution in humans, we could expect the increment of the CBD bioavailability by nanoemulsification to be higher than that observed in the present study (65%).…”

Section: Discussionmentioning

confidence: 99%

Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol

Nakano

Tajima

Sugiyama

et al. 2019

Med Cannabis Cannabinoids

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Background: Cannabidiol (CBD) is highly lipophilic, and its oral bioavailability is known to be very low in humans. In this study, we developed a novel nanoemulsion preparation of CBD (CBD-NE) to improve the poor solubility and absorption of CBD. The pharmacokinetic profiles of CBD in rats were evaluated after oral administrations of CBD oil and CBD-NE, and the effect of bile secretion on CBD absorption was also evaluated. Methods: The CBD-NE formulation developed in this study consisted of vitamin E acetate, ethanol, Tween-20, and distilled water (1.7/3.8/70/24.5, w/w%). A CBD oil formulation (CBD oil, control) 100 mg/kg or CBD-NE 50 mg/kg was orally administered to rats, and the blood samples were collected over time. Moreover, the CBD oil or CBD-NE was orally administered to bile-fistulated rats, and the pharmacokinetic profiles of CBD were also evaluated. CBD concentrations in plasma were measured using LC-MS/MS. Results: The particle size of CBD-NE was 35.3 ± 11.8 nm. Mean T_max of CBD-NE was shortened significantly by the factor of 3 (from 8.00 to 2.40 h, p < 0.001) and AUC_0–_∞/dose increased by 65% (from 0.272 ± 0.045 to 0.448 ± 0.087 h L/kg) compared with CBD oil. AUC_0–_∞/dose and C_max/dose after oral administration of CBD oil were significantly reduced by the factor of 27 and 23 (p < 0.05 and p < 0.01), respectively, in bile-fistulated rats compared with the untreated rats. In contrast, all pharmacokinetic parameters after oral administration of CBD-NE were not significantly different between the untreated and bile-fistulated rats. Therefore, these results demonstrated that conventional CBD oil formulation but not CBD-NE requires bile-mediated micelle formation. Conclusions: The novel NE formulation developed in this study successfully improved the absorption of CBD regardless of bile secretion. The newly developed oral CBD-NE preparation could be useful to achieve a more stable and quicker onset of action by CBD.

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“…Metabolism of CBD showed biotransformation routes typically observed for phytocannabinoids [44,45]. Although different metabolic pathways have been observed in different animal species, including human, overall CBD metabolism displays common features.…”

Section: Cbd Pharmacologymentioning

confidence: 99%

Cannabidiol: A Promising Drug for Neurodegenerative Disorders?

Iuvone

Esposito

Filippis

et al. 2009

CNS Neuroscience & Therapeutics

188

110

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Neurodegenerative diseases represent, nowadays, one of the main causes of death in the industrialized country. They are characterized by a loss of neurons in particular regions of the nervous system. It is believed that this nerve cell loss underlies the subsequent decline in cognitive and motor function that patients experience in these diseases. A range of mutant genes and environmental toxins have been implicated in the cause of neurodegenerative disorders but the mechanism remains largely unknown. At present, inflammation, a common denominator among the diverse list of neurodegenerative diseases, has been implicated as a critical mechanism that is responsible for the progressive nature of neurodegeneration. Since, at present, there are few therapies for the wide range of neurodegenerative diseases, scientists are still in search of new therapeutic approaches to the problem. An early contribution of neuroprotective and antiinflammatory strategies for these disorders seems particularly desirable because isolated treatments cannot be effective. In this contest, marijuana derivatives have attracted special interest, although these compounds have always raised several practical and ethical problems for their potential abuse. Nevertheless, among Cannabis compounds, cannabidiol (CBD), which lacks any unwanted psychotropic effect, may represent a very promising agent with the highest prospect for therapeutic use.

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Metabolism of cannabidiol by the rat

Cited by 14 publications

References 15 publications

Conversion of Cannabidiol (CBD) into Psychotropic Cannabinoids Including Tetrahydrocannabinol (THC): A Controversy in the Scientific Literature

Conversion of Cannabidiol (CBD) into Psychotropic Cannabinoids Including Tetrahydrocannabinol (THC): A Controversy in the Scientific Literature

Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol

Cannabidiol: A Promising Drug for Neurodegenerative Disorders?

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Metabolism of cannabidiol by the rat

Cited by 14 publications

References 15 publications

Conversion of Cannabidiol (CBD) into Psychotropic Cannabinoids Including Tetrahydrocannabinol (THC): A Controversy in the Scientific Literature

Conversion of Cannabidiol (CBD) into Psychotropic Cannabinoids Including Tetrahydrocannabinol (THC): A Controversy in the Scientific Literature

Development of a Novel Nano­emulsion Formulation to Improve Intestinal Absorption of Cannabidiol

Cannabidiol: A Promising Drug for Neurodegenerative Disorders?

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Development of a Novel Nanoemulsion Formulation to Improve Intestinal Absorption of Cannabidiol