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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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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cited_by cdi_FETCH-LOGICAL-c4356-c3a39bb21a645607d1d3d31006cfaf5e7e40c4489d7c564a5c2894f302f679e23
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creator Mannila, Janne
Järvinen, Tomi
Järvinen, Kristiina
Jarho, Pekka
description 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
doi_str_mv 10.1002/jps.20766
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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&lt;0.05) higher than that of plain CBD. The absorption of CBD (AUC0–300min) decreased in the following order: sublingual ethanolic CBD solution (420±120 ng×min/mL; mean±SD; n=4) &gt; sublingual solid CBD/β-CD complex (270±120 ng×min/mL) &gt; 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. 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Pharm. Sci</addtitle><description>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&lt;0.05) higher than that of plain CBD. The absorption of CBD (AUC0–300min) decreased in the following order: sublingual ethanolic CBD solution (420±120 ng×min/mL; mean±SD; n=4) &gt; sublingual solid CBD/β-CD complex (270±120 ng×min/mL) &gt; 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. 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source Wiley Online Library Journals; Elsevier ScienceDirect Journals
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
title Precipitation Complexation Method Produces Cannabidiol/β-Cyclodextrin Inclusion Complex Suitable for Sublingual Administration of Cannabidiol
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