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Allicin cyclodextrin clathrate compound, formulation and its preparation method

A cyclodextrin inclusion compound and allicin technology, which is applied in the field of medicine, can solve problems affecting the quality of medication and patient safety, poor stability, and irritation of human mucous membranes. The effect of high content

Inactive Publication Date: 2005-01-19
毛友昌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the existing dosage forms of allicin are allicin injection (2ml: 30mg, 5ml: 60mg), allicin enteric-coated tablets, allicin enteric-coated capsules, allicin is an oily liquid, volatile, almost insoluble in water, stable Poor sex, specific garlic smell, irritating to human mucous membranes, allicin injection needs to add solubilizer and stabilizer to increase its solubility and stability in water, the injection is painful when injected intramuscularly, Intravenous infusion must be diluted, the operation is troublesome, and it is easy to cause liquid pollution and medical errors, affecting the quality of medication and patient safety, and making it into cyclodextrin inclusion complexes can not only increase its water solubility, stability, Cover bad smell, reduce irritation, and solidify liquid medicine, which is convenient for preparation processing

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0021] Example 1: Preparation of allicin β-cyclodextrin inclusion compound: weigh allicin and β-cyclodextrin according to the above ratio; add appropriate amount of water / ethanol and water, heat, stir / slowly drop under ultrasound The above-mentioned allicin solution was stirred / sonicated until the specified time, refrigerated for 24 hours, suction filtered, washed, and the precipitate was dried at low temperature to obtain the product.

Embodiment 2

[0022] Example 2: Preparation of allicin hydroxypropyl-β-cyclodextrin inclusion compound: weigh allicin and hydroxypropyl-β-cyclodextrin according to the above ratio, and use an appropriate amount of ethanol / absolute ethanol solution for allicin Standby; add appropriate amount of hydroxypropyl-β-cyclodextrin to dissolve, slowly add the above-mentioned allicin solution dropwise under stirring / ultrasound, continue to stir / ultrasound until the specified time, filter with a 0.45μ membrane and then use a 0.22μ membrane After filtering, the resulting solution is vacuum-dried / spray-dried / freeze-dried to obtain a white powder, that is, allicin hydroxypropyl-β-cyclodextrin inclusion compound.

Embodiment 3

[0023] Example 3: Preparation of allicin hydroxyethyl-β-cyclodextrin inclusion compound: weigh allicin and hydroxyethyl-β-cyclodextrin according to the above ratio, and use appropriate amount of ethanol / absolute ethanol solution for allicin Standby; add appropriate amount of hydroxypropyl-β-cyclodextrin to dissolve, slowly add the above-mentioned allicin solution dropwise under stirring / ultrasound, continue to stir / ultrasound until the specified time, filter with a 0.45μ membrane and then use a 0.22μ membrane After filtering, the resulting solution is vacuum-dried / spray-dried / freeze-dried to obtain a white powder, that is, allicin hydroxyethyl-β-cyclodextrin inclusion compound.

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PUM

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Abstract

The invention discloses a garlicin cyclodextrin clathrate compound, preparation and the process for preparing same, wherein the allicin, cyclodextrin or their derivatives (such as beta-cyclodextrin, hydroxypropyl-beta-cyclodextrin) can be used for preparing garlicin cyclodextrin clathrate compound, which can be used for preparing various preparations of different oral preparation, suppositorium, spray, and injection.

Description

technical field [0001] The present invention relates to the field of medical technology, specifically, it uses cyclodextrin or its derivatives to form inclusion complexes with allicin or adds cyclodextrin or its derivatives to improve the solubility and stability of allicin in water and reduce irritation. Sex, mask bad smell, thus make allicin cyclodextrin inclusion compound and its preparation. Background technique [0002] Garlic is the underground bulb of the Allium genus garlic in the Liliaceae family. Spicy in taste, warm in nature, it belongs to the spleen, stomach, and lung meridians, and has the effects of detoxifying, killing insects, reducing swelling, and stopping dysentery. It has been used as a folk medicine in my country for thousands of years. Allicin is the main active ingredient in the volatile oil of garlic. Modern studies believe that allicin has strong antibacterial, antiprotozoal, trichomonas, antiviral, antitumor, antioxidative,...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/105A61K47/40A61P1/16A61P9/10A61P31/00A61P33/02A61P35/00A61P43/00
Inventor 毛友昌毛晓敏
Owner 毛友昌
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