cbd cyclodextrin complex

A peer reviewer from Journal of Molecular Liquids said the study was “well organized and described the concept of complexation very well”.

Moreover, the water solubility of CBD in CBD/β-CD IC and CBD/DM-β-CD IC was significantly increased to 0.395 and 14.118 μg/mL, which was enhanced by 17-fold and 614-fold respectively at such a high LE, and the in vitro dissolution rate of CBD was also promoted.

Moreover, the results of molecular docking further showed that CBD was encapsulated successfully.

Cyclodextrins ( CDs) are useful materials to improve the solubility of poorly water-soluble molecules. Therefore, the researchers used β-cyclodextrin (β-CD) and 2, 6-di-O-methyl-β-cyclodextrin (DM-β-CD) to prepare CBD/ β-CD IC and CBD/ DM-β-CD IC by freeze-drying method to improve the water solubility and dissolution rate of CBD.

T he antioxidant activity of CBD was improved after encapsulation. Significantly, the ABTS free radical scavenging ability of the ICs was better than that of Vitamin C.

CBD has a wide variety of biological activities, and it is one of the phytocannabinoids from Cannabis sativa L (Hemp) . However, due to the poor aqueous solubility, its applications in food, cosmetic, and pharmaceutical fields are limited.

Job’s plot and phase solubility study revealed that CBD formed ICs with β-CD and DM-β-CD at a stoichiometric ratio of 1:1. The thermodynamics analysis demonstrated that the inclusion process was spontaneous and endothermic. The loading efficiency (LE) of CBD/ β-CD IC and CBD/ DM-β-CD IC was 20.4% and 17.7%, respectively, while the complexation efficiency (CE) was 92.4% and 90.8% respectively.

The study was published in Journal of Molecular Liquids on April 8 (DOI: 10.1016/j.molliq.2021.116070 ).

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The researchers hoped that this work could provide theoretical and experimental support for expanding the application of cannabidiol .

and co-administration of small amounts of water-soluble polymer (HPMC) enhances the complexation between HP-13-CD and THC. In addition, Song et al.
(2000) and Porcella et al. (2001) have recently used HP-13-CD to solubilize the aminoalkylindol derivative WIN-55212 in topical ophthalmic formulations.
SUMMARY OF THE INVENTION
The present invention is directed to a novel use of a complex between a specific group of cyclodextrins and cannabinoids. Specifically, the invention relates to a complex of a cyclodextrin selected from the group consisting of a-CD, 13-CD
and 7-CD, and a cannabinoid selected from the classical cannabinoid-group consisting of cannabinol, tetrahydrocannabinol and cannabidiol.
Specifically the present invention is directed to the use of the said complex for the preparation of a pharmaceutical composition for sublingual or buccal administration. The invention is also directed to pharmaceutical compositions containing such a complex which are intended for sublingual or buccal administration, for example in the form of a tablet, capsule, chewing gum, lozenge or pill.

7 The therapeutic dose to be given to a patient in need of treatment will vary depending i.a. on the body weight and age of the patient, the particular condition being treated as well as the manner of administration and are easily determined by a person skilled in the art. Generally a concentration of 0.1 mg to 500 mg cannabinoid, typically 0.1 mg to 50 mg per unit dose, to be given for example 1 to 4 times a day, would be suitable for most purposes.
The following examples illustrate the invention without limiting the same in any way.

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In this example the effect of natural 13-CD on the dissolution characteristics of CBD
have been described.
A powder containing a CBD/13-CD inclusion complex was prepared by the precipitation method. In this method a methanol solution of CBD was added dropwise to an aqueous 13-CD solution and after equilibration the white precipitate (CBD/13-CD inclusion complex) was isolated and dried. The HPLC analysis of the powder showed that 9.1 mg of the powder contained 1.0 mg of CBD. All the following dissolution experiments were made in 2% RM-I3-CD dissolution medias (pH 6.6) to ensure the free solubility of CBD.
Figure 1 shows the dissolution profile (dissolved CBD as a function of time) of CBD from a gelatine capsule containing 1.0 mg of pure CBD and 99 mg of lactose (Mean + SD, n=6). Figure 2 shows the same data with a capsule containing 9.1 mg of natural 13-CD/CBD-complex (equivalent to lmg of THC) and 90.9 mg of lactose (Mean + SD, n=4).
Figures 1 and 2 show that the complexation of CBD with natural 13-CD
significantly increases the dissolution rate of CBD. With a 13-CD/CBD
formulation,