Water-soluble cannabidiol nano preparation based on cyclodextrin carrier and preparation method thereof

A technology of cannabidiol nano and cannabidiol, which is applied in the direction of medical preparations of non-active ingredients, pharmaceutical formulas, active ingredients of hydroxyl compounds, etc., can solve the problem of inability to achieve on-demand configuration, unsatisfactory solubilization effect, and limited diversity In order to improve the stability and bioavailability, increase the water solubility of the drug, and reduce the irritation and adverse reactions

Inactive Publication Date: 2020-04-14
云南省农业科学院经济作物研究所 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the strong hydrophobicity of cannabidiol, it is easy to decompose when exposed to light, and its bioavailability is low, which limits its diversified applications in the fields of medicine, food, cosmetics, etc.
So far, although some water-soluble cannabidiol inclusion compounds have been reported, their inclusion efficiency is low. Calculated based on CBD content, the solubilization effect is not ideal and cannot be configured on demand

Method used

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  • Water-soluble cannabidiol nano preparation based on cyclodextrin carrier and preparation method thereof
  • Water-soluble cannabidiol nano preparation based on cyclodextrin carrier and preparation method thereof
  • Water-soluble cannabidiol nano preparation based on cyclodextrin carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: Preparation of Water-Soluble Cannabidiol Nano-Preparation Based on Hydroxypropyl-β-cyclodextrin

[0021] Add 25mL of 1mmol / mL hydroxypropyl-β-cyclodextrin aqueous solution into a 100mL reaction bottle (distilled water as solvent water), then add 100mmol cannabidiol, stir the reaction at 50°C at 200rpm in the dark for 30d, and then use The undissolved solids were removed by filtration through a 0.1 μm microporous membrane, and the filtrate was vacuum-dried (100Pa, 12h) to obtain a white powder. The water-soluble cannabidiol nano-preparation of cyclodextrin (according to the amount of substances, the preparation is 50% cannabidiol and 50% cyclodextrin, and the particle size obtained by a particle size analyzer is 0.5-1.2nm. 1 H NMR data, 500MHz, D 2 O: δ0.5–2.5(H of CBD and CD, 50H),3.0–4.0(H of CD and CBD,39H),4.83–4.95(H of CD,7H),5.0–5.2(H of CBD,2H )). pass 1 H NMR data conversion can be obtained, the solubility of cannabidiol in water is 157.23mg / mL. ...

Embodiment 2

[0022] Example 2 Preparation of Water-Soluble Cannabidiol Nano-Preparation Based on γ-cyclodextrin

[0023] Add 1mmol / mL γ-cyclodextrin N, N-dimethylformamide-water solution 30mL in a 150mL reaction flask (the solvent is a mixed solvent of analytically pure N,N-dimethylformamide and distilled water, analytically pure N, N-dimethylformamide and distilled water v:v=1:4), then add 3mmol / mL cannabidiol acetone-water suspension 10mL (solvent is the mixed solvent of analytical pure acetone and distilled water, analytical pure acetone and Distilled water (v:v=4:1), stirred at 500rpm in the dark for 3 days at 25°C to complete the reaction, then filtered through a 0.1μm microporous membrane to remove undissolved solids, and the filtrate was vacuum-dried (100Pa, 12h ) to obtain a white powder, and the NMR test results show that it is a water-soluble cannabidiol nano-preparation based on γ-cyclodextrin (according to the amount of substance, the preparation is 12% cannabidiol, 88% cyclode...

Embodiment 3

[0024] Example 3: Preparation of water-soluble cannabidiol nano-preparation based on α-cyclodextrin

[0025]Add 1mmol / L α-cyclodextrin methanol-water solution 10mL in a 50mL reaction bottle (the solvent is a mixed solvent of analytically pure methanol and distilled water, v:v=1:4 for analytically pure methanol and distilled water), then add 10mmol / mL Cannabidiol dimethyl sulfoxide-water suspension 5mL (the solvent is a mixed solvent of analytical pure dimethyl sulfoxide and distilled water, and the v:v=1:1 of analytical pure dimethyl sulfoxide and distilled water), in Stir the reaction at 700rpm in the dark at 30°C for 7 days, then filter through a 0.1μm microporous membrane to remove undissolved solids, and vacuum-dry the filtrate (100Pa, 12h) to obtain a white powder. The NMR test results show that it is based on α- Water-soluble cannabidiol nano-preparation of cyclodextrin (according to the amount of substances, the preparation is composed of 20% cannabidiol and 80% cyclode...

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Abstract

The invention discloses a water-soluble cannabidiol nano preparation based on a cyclodextrin carrier and a preparation method thereof. In terms of the amount of substances, the preparation is preparedfrom 1-50% of cannabidiol and 99-50% of cyclodextrin. The preparation has good water solubility, stability and bioavailability. In terms of the solubility of cannabidiol in water, the preparation hassolubility of 0.046-157.23mg/mL, and water-soluble cannabidiol nano-preparations with different concentrations can be prepared according to needs. The preparation method includes: adding cannabidiolor a suspension into a cyclodextrin solution, carrying out reaction under proper conditions, and performing filtering, freezing or vacuum drying. The preparation method is simple, mild in conditions and easy for industrial production, and can solve the problem that application of cannabidiol in drugs, foods, cosmetics and other fields is limited due to extremely low solubility of cannabidiol in water.

Description

technical field [0001] The invention belongs to the technical field of preparation preparation, and in particular relates to a water-soluble cannabidiol nano preparation based on a cyclodextrin carrier and a preparation method thereof. Background technique [0002] Marijuana (Cannabis sativa L.) is an annual herb plant of the Cannabis family (Cannabinaceca). Its roots, stems, flowers, leaves, and seeds can be used as medicine. Hydrocannabinol (Tetrahydrocannabinol, THC), cannabidiol (Cannabidiol, CBD), cannabinol (Cannabinol, CBN), cannabigerol (Cannabigerol, CBG) and cannabichromene (CBC), among which THC The highest content of phenols and cannabidiol (about 90% of phenols). At present, the research on cannabidiol is the most extensive and in-depth. According to a large number of literature reports, cannabidiol shows good anti-tumor activity in tumor cells such as breast cancer, prostate cancer, glioma and leukemia; it has good antibacterial effect on Gram-positive bacter...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/69A61K31/05A61P35/00A61P35/02A61P31/04
CPCA61K9/5161A61K31/05A61K47/6951A61P31/04A61P35/00A61P35/02
Inventor 吕品郭孟璧郭鸿彦杨明郭蓉许艳萍陈璇张庆滢潘宗兵
Owner 云南省农业科学院经济作物研究所
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