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Preparation method of sulforaphane inclusion compound

A technology of sulforaphane and clathrate, applied in the field of biomedicine, can solve the problems of difficult filtration and collection of products, complicated process and high cost

Active Publication Date: 2021-11-26
SHENZHEN F&S BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the above cyclodextrin cryoprecipitation method can obtain the stabilized product of sulforaphane—sulforaphane α-cyclodextrin inclusion complex, the cryoprecipitation method itself still has problems such as many procedures, large equipment investment, and high cost. Not suitable for industrial scale production
In this method, in order to cause the inclusion of cyclodextrin and sulforaphane in the solution to separate out due to the difference in solubility at different temperatures, the entire production process needs to go through multiple processes such as dissolution and inclusion, cooling and precipitation, filtration, drying, and solution recycling. The whole process takes a long time and requires a lot of equipment investment
Moreover, when α-cyclodextrin is cooled and precipitated at low temperature, due to its own properties, it is easy to form fine amorphous precipitates, which makes it difficult to filter and collect the product, resulting in large production losses; at the same time, in order to repeatedly use the saturated solution of α-cyclodextrin after precipitation, it is necessary to Remove impurities in saturated solution, which makes the process more complicated

Method used

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  • Preparation method of sulforaphane inclusion compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Preparation of Sulforaphane α-Cyclodextrin Inclusion Complex (A)

[0024] (1) Mixing: Prepare 1L sulforaphane aqueous solution (containing 18.4g sulforaphane, self-made) and 3L α-cyclodextrin suspension (containing 2000g α-cyclodextrin, purity 99%; sulforaphane mole : Cyclodextrin moles=1:20) uniformly mixed to obtain 4L sulforaphane α-cyclodextrin mixture;

[0025] (2) Spray-drying: After spray-drying the above mixed solution at 170° C., the sulforaphane α-cyclodextrin inclusion complex powder was collected.

[0026] Take 0.100 g of the above powder, quantitatively dissolve it in 10 mL of water, detect the concentration of sulforaphane by HPLC, and find that sulforaphane accounts for 0.995% of the solid content. (Sulforaphane accounts for solid content%=sulforaphane concentration (mg / mL)×sample dissolved volume (mL) / sample mass (mg)×100%)

[0027] Another 0.100g of the above powder was washed with 10mL of dichloromethane to remove the unincluded sulforaphane on the s...

Embodiment 2

[0030]Preparation of Sulforaphane α-Cyclodextrin Inclusion Complex (B)

[0031] (1) Mixing: Prepare 1L sulforaphane aqueous solution (containing 34.0g sulforaphane, self-made) and 3L α-cyclodextrin suspension (containing 1870g α-cyclodextrin, purity 99%, sulforaphane molar : Cyclodextrin molar number=1:10) uniformly mixed to obtain 4L sulforaphane α-cyclodextrin mixed solution;

[0032] (2) Spray drying: After spray drying the above mixed solution at 170° C., the powder was collected.

[0033] As described in Example 1, it is measured that sulforaphane accounts for 1.96% of the solid content of the powder. After washing with dichloromethane to remove the unincluded sulforaphane on the surface, it is measured that sulforaphane accounts for 1.89% of the solid content of the powder. The inclusion rate of prime is 96%.

Embodiment 3

[0035] Preparation of Sulforaphane α-Cyclodextrin Inclusion Complex (C)

[0036] (1) Mixing: Prepare 1L sulforaphane aqueous solution (containing 62.5g sulforaphane, self-made) and 3L α-cyclodextrin suspension (containing 1750g α-cyclodextrin, purity 99%, sulforaphane mole : Cyclodextrin molar number=1:5) uniformly mixed to obtain 4L sulforaphane α-cyclodextrin mixed solution;

[0037] (2) Spray drying: After spray drying the above mixed solution at 170° C., the powder was collected.

[0038] As described in Example 1, it is measured that sulforaphane accounts for 3.74% of the solid content of the powder. After washing with dichloromethane to remove the unincluded sulforaphane on the surface, it is measured that sulforaphane accounts for 3.60% of the solid content of the powder. The inclusion rate of prime is 96%.

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Abstract

The invention relates to a preparation method of a sulforaphane α-cyclodextrin compound inclusion compound, the inclusion compound prepared by the preparation method and use thereof. The present invention adopts spray drying method to prepare sulforaphane α-cyclodextrin compound inclusion compound, and in the inclusion compound, the molar ratio of sulforaphane to α-cyclodextrin compound is 1:0.8~1:20 . The preparation method of the invention overcomes the problems of many process steps and high actual production cost in the prior art, and is easy for large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a preparation method of sulforaphane alpha-cyclodextrin inclusion compound and the inclusion compound prepared by the preparation method. The present invention also relates to the use of said clathrate in the preparation of products for cancer chemoprevention and treatment. Background technique [0002] According to the 2014 annual report of the World Health Organization, cancer is the main cause of global morbidity and death, poses a huge threat to people's life and health, and brings a heavy economic burden to social development. In the long process of fighting cancer, the concept of cancer chemoprevention was proposed in 1976. Cancer chemoprevention refers to the use of natural or synthetic chemical substances to prevent, slow down or reverse the development of cancer strategies. Sulforaphane (SFN), also known as sulforaphane, chemically named 1-isothiocyanate-4-methan...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K31/26A61P35/00A23L33/10A23L33/125
CPCA23V2002/00A61K31/26A23L33/10A23L33/125A23V2200/308
Inventor 李晓龙朱志鹏李欣
Owner SHENZHEN F&S BIO TECH