A meta-opinion: cannabinoids delivered to oral mucosa by a spray for systemic absorption are rather ingested into gastro-intestinal tract: the influences of fed / fasting states

@article{Itin2019AMC,
  title={A meta-opinion: cannabinoids delivered to oral mucosa by a spray for systemic absorption are rather ingested into gastro-intestinal tract: the influences of fed / fasting states},
  author={Constantin Itin and Abraham J. Domb and Amnon Hoffman},
  journal={Expert Opinion on Drug Delivery},
  year={2019},
  volume={16},
  pages={1031 - 1035}
}
ABSTRACT Introduction: Sativex® spray is clinically utilized to deliver delta9-tetrahydrocannabinol and cannabidiol to oral mucosa for systemic absorption. We challenge the consensus that the mechanism of absorption following the oro-mucosal application occurs via the buccal tissue. Areas covered: Correctness of the consensus of this absorption pathway arose when reviewing publications regarding the influence fed versus fasting states have on pharmacokinetics of these cannabinoids administered… 
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References

SHOWING 1-10 OF 23 REFERENCES
Influence of Hepatic and Intestinal Cytochrome P4503A Activity on the Acute Disposition and Effects of Oral Transmucosal Fentanyl Citrate
Background: Oral transmucosal fentanyl citrate (OTF) was developed to provide rapid analgesia and is specifically approved for treating breakthrough cancer pain. Fentanyl in OTF is absorbed across…
Piperine‐pro‐nanolipospheres as a novel oral delivery system of cannabinoids: Pharmacokinetic evaluation in healthy volunteers in comparison to buccal spray administration
A Systematic Review on the Pharmacokinetics of Cannabidiol in Humans
TLDR
The paucity in data and some discrepancy in the pharmacokinetics of cannabidiol are highlighted, despite its widespread use in humans, and robust data from a variety of formulations is required.
Effect of abdominal surgery on the intestinal absorption of lipophilic drugs: possible role of the lymphatic transport.
PTL401, a New Formulation Based on Pro-Nano Dispersion Technology, Improves Oral Cannabinoids Bioavailability in Healthy Volunteers.
Drug recovery following buccal absorption of propranolol.
TLDR
Large amounts of propranolol were recoverable from the buccal mucosa; recovery was biexponential and the amount recovered depended on the time allowed for absorption and on the pH of buffers used for recovery.
A membrane model of the human oral mucosa as derived from buccal absorption performance and physicochemical properties of the β‐blocking drugs atenolol and propranolol
TLDR
A new compartmental diffusional model that includes membrane storage and a hypothetical ‘aqueous pH‐buffering surface system’ allowed a more exhaustive interpretation to be made and showed that propranolol in its unionized form is much more lipophilic than atenolol, both drugs being bases with a similar pKa.
Oral Mucosal Drug Delivery and Therapy
TLDR
This volume provides a comprehensive overview of the current issues facing scientists working on delivering drugs locally and systemically via the membranes that line the mouth, and provides insights into the in vitro and in vivo methods available to assess drug permeability and retention.
Human Cannabinoid Pharmacokinetics
  • M. Huestis
  • Biology, Chemistry
    Chemistry & biodiversity
  • 2007
TLDR
The cardiovascular and subjective effects of cannabis are blocked by rimonabant, the first CB-1 cannabinoid-receptor antagonist, documenting thatCB-1 receptors mediate these effects of smoked cannabis in humans.
Effect of food on the pharmacokinetics of dronabinol oral solution versus dronabinol capsules in healthy volunteers
TLDR
Dronabinol oral solution may offer therapeutic benefit to patients, given its rapid and lower interindividual absorption variability versus dronabinian capsule, and an appreciable food effect was observed.
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