Precipitation Complexation Method Produces Cannabidiol/β-Cyclodextrin Inclusion Complex Suitable for Sublingual Administration of Cannabidiol

In the present study, the precipitation complexation method was used to prepare a complex of cannabidiol (CBD) with β-CD. The effect of β-CD-complexation on the sublingual absorption of CBD was studied in rabbits. A solid CBD/β-CD inclusion complex was prepared by precipitation and the effect of com...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2007-02, Vol.96 (2), p.312-319
Main Authors: Mannila, Janne, Järvinen, Tomi, Järvinen, Kristiina, Jarho, Pekka
Format: Article
Language:English
Subjects:
Absorption
Administration, Oral
Administration, Sublingual
Animals
beta-Cyclodextrins - administration & dosage
beta-Cyclodextrins - chemistry
Biological and medical sciences
Biological Availability
buccal
Cannabidiol - administration & dosage
Cannabidiol - chemistry
Cannabidiol - pharmacokinetics
Chemical Precipitation
cyclodextrins
Drug Compounding
Ethanol - chemistry
Female
General pharmacology
Male
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
preformulation
Rabbits
Solubility
transmucosal drug delivery
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Summary:In the present study, the precipitation complexation method was used to prepare a complex of cannabidiol (CBD) with β-CD. The effect of β-CD-complexation on the sublingual absorption of CBD was studied in rabbits. A solid CBD/β-CD inclusion complex was prepared by precipitation and the effect of complex formation on the dissolution rate of CBD was studied. The absorption of CBD (a 250 µg/kg dose of CBD in all formulations) after sublingual administration of solid CBD/β-CD complex and ethanolic CBD solution, and after oral administration of ethanolic CBD solution, was studied in vivo in rabbits. The dissolution rate of solid CBD/β-CD complex in vitro was significantly (p sublingual solid CBD/β-CD complex (270±120 ng×min/mL) > oral ethanolic CBD solution (concentrations in plasma below the quantitation limit). The results demonstrate that sublingual administration of a solid CBD/β-CD complex enhances the absorption of CBD in rabbits when compared to oral administration of ethanolic CBD. Furthermore, the solid CBD/β-CD complex may provide an alternative formulation for sublingual administration of CBD. ©2006 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 96:312–319, 2007
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.20766