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Allyl isothiocyanate-beta-cyclodextrin inclusion compound

A technology of cyclodextrin inclusion complex and isothiocyanate is applied in directions such as pharmaceutical combinations, ester active ingredients, and non-active ingredients medical preparations, etc. Bioavailability, ease of transport and preservation of use

Inactive Publication Date: 2013-12-25
上海海虹实业(集团)巢湖今辰药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Acute and chronic toxicity experiments, teratogenicity, carcinogenicity, and mutagenicity experiments have all proved that its use is safe and non-toxic, so β-cyclodextrin inclusion technology has attracted much attention in the field of traditional Chinese medicine preparations. At present, there are many domestic and foreign researches on β-cyclodextrin. There are literature reports on cyclodextrin inclusion technology, but there is no public report on the inclusion of allyl isothiocyanate-β-CD cyclodextrin

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1: Preparation of allyl isothiocyanate β-cyclodextrin inclusion compound

[0013] Add allyl isothiocyanate (100mg) dissolved in an organic solvent (absolute ethanol or acetone) to the aqueous solution of β-cyclodextrin, at a speed of 100-300r / min and a temperature of 30°C-60°C Stir at constant temperature for 1-3 hours, filter through a 0.22 μm microporous membrane, collect the filtrate, and dry in vacuum at low temperature for 5-6 hours to obtain the allyl isothiocyanate-β-cyclodextrin inclusion compound. Detected by ultraviolet light detection method, the content of allyl isothiocyanate in the obtained clathrate is calculated, and the inclusion yield is calculated (actually measured content of allyl isothiocyanate*inclusion compound yield / isothiocyanate Allyl ester input).

[0014] 1. Determine the proof that the product obtained in Example 1 forms an inclusion compound:

[0015] (1) Use thin-layer chromatography to determine whether clathrates are formed: ...

Embodiment 2

[0021] Example 2: Preparation of allyl isothiocyanate β-cyclodextrin inclusion compound

[0022] Dissolve 100mg of allyl isothiocyanate in 150mL ethanol solution to obtain allyl isothiocyanate dissolved in ethanol solution, set aside, then take 10g of β-cyclodextrin and dissolve in 1000mL of distilled water, magnetic stirring conditions at room temperature to Add allyl isothiocyanate ethanol solution to the saturated aqueous solution of β-cyclodextrin, continue to stir for 2 hours, let it stand overnight, evaporate the ethanol under reduced pressure, filter, and dry the filtrate under reduced pressure and low temperature to obtain allyl isothiocyanate The β-cyclodextrin inclusion compound is detected by ultraviolet spectroscopic detection method, and the content of allyl isothiocyanate in the obtained inclusion compound.

Embodiment 3

[0023] Example 3: Preparation of allyl isothiocyanate β-cyclodextrin inclusion compound

[0024] Dissolve 100mg of allyl isothiocyanate in 150mL of acetone solution to obtain allyl isothiocyanate dissolved in acetone solution, set aside, then take 10g of β-cyclodextrin dissolved in 1000mL of distilled water, ultrasonic vibration (ultrasonic frequency Add allyl isothiocyanate acetone solution to the β-cyclodextrin saturated aqueous solution under the condition of 40-60KHZ), continue ultrasonication for 1 hour, let stand overnight, evaporate ethanol under reduced pressure, filter, and dry the filtrate under reduced pressure and low temperature. It is confirmed by thin-layer chromatography that the inclusion compound of allyl isothiocyanate β-cyclodextrin is obtained, and the content of allyl isothiocyanate in the inclusion compound is detected by ultraviolet spectrum detection.

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PUM

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Abstract

The invention discloses an allyl isothiocyanate-beta-cyclodextrin inclusion compound which comprises allyl isothiocyanate, beta-cyclodextrin, absolute ethyl alcohol and water for injection, wherein the mass ratio of the allyl isothiocyanate and the beta-cyclodextrin is 1:(1-100). The allyl isothiocyanate-beta-cyclodextrin inclusion compound can be prepared into medicine with the dosage form such as powder injection, injection, oral preparation, external gel, ointment, spray or naristillae together with a pharmaceutically acceptable carrier. The inclusion compound yield is taken as an inspection index, and the technology of the allyl isothiocyanate-beta-cyclodextrin inclusion compound is selected in an optimized way by adopting a single factor and an orthogonal test; furthermore, allyl isothiocyanate is covered by the beta-cyclodextrin, so that the solubility of the allyl isothiocyanate can be increased, the bioavailability is improved, the spicy taste of the allyl isothiocyanate is covered up by the beta-cyclodextrin, the irritation to the organism is reduced, the medicine release is adjusted and controlled, and the allyl isothiocyanate-beta-cyclodextrin inclusion compound is convenient to transport, store and use.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, and discloses an allyl isothiocyanate-β-cyclodextrin inclusion compound, more specifically, an allyl isothiocyanate-β-cyclodextrin inclusion compound of the present invention, Increase the solubility of allyl isothiocyanate, improve bioavailability, mask the pungent taste of allyl isothiocyanate, reduce the irritation to the body, adjust and control drug release, and facilitate transportation and storage. Background technique [0002] AllyL isothiocyanate (AITC) is the main taste substance of mustard oil. Due to its unique taste and antibacterial properties, recent studies have found that it can inhibit the growth of cancer cells and can also replace methyl bromide in agriculture. As a soil disinfectant, allyl isothiocyanate has broad application prospects in food additives, food antibacterial and antiseptic, medical anticancer and soil disinfection. However, allyl isothiocyanate's str...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/48A61K31/26A61P35/00
Inventor 陈卫东朱婷婷方国民张先文林彤远罗晴蔡晓蕾王雷
Owner 上海海虹实业(集团)巢湖今辰药业有限公司
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