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Method for preparing water-soluble soybean aglycon and its applications

A daidzein and water-soluble technology, which is applied in the field of preparing water-soluble daidzein, can solve the problems of poor water solubility, restriction of administration routes and dosage forms, and insolubility, etc., and achieves the effects of stable quality, advanced and convenient, and low manufacturing cost

Inactive Publication Date: 2003-07-23
沈阳海德医药化工有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Daidzein is an isoflavone compound, and its own structural characteristics determine that there is a relatively large shortcoming and deficiency, that is, the water solubility is extremely poor and cannot be dissolved in water, resulting in extremely low bioavailability of oral preparations, which limits the The route of administration and dosage form greatly affect the clinical efficacy and clinical application range

Method used

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  • Method for preparing water-soluble soybean aglycon and its applications
  • Method for preparing water-soluble soybean aglycon and its applications
  • Method for preparing water-soluble soybean aglycon and its applications

Examples

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Embodiment 1

[0029] The present invention will be further illustrated by embodiments with reference to the accompanying drawings. However, the following examples are only examples of the present invention, and do not represent the scope of rights limited by the present invention. The scope of the rights is subject to the claims. Example 1: One of the preparation methods of water-soluble daidzein

[0030] Take 5g of daidzein, add sodium hydroxide solution to dissolve, adjust the pH to 11, filter, add 100ml of acetone, stir evenly, after standing for 4 hours, filter, wash three times with a little acetone, and reduce the resulting precipitate at 40°C under reduced pressure After drying to constant weight, 3.6 g of white crystalline powder is obtained. Differential thermal analysis shows that it contains two molecules of crystal water, see attached image 3 , 4 , Elemental analysis results: C 50.32%; H 3.62%; Na 12.67% [Daidzein Sodium Dihydrate, Theoretical Value is C 53.90%; H 3.62%; Na 13.75%]...

Embodiment 2

[0046] Take 5g of daidzein, add sodium hydroxide solution to dissolve, adjust the pH to 10, filter, add 100ml of isopropanol, stir evenly, after standing for 3 hours, filter, wash with a little isopropanol three times, the resulting precipitate is Dry under reduced pressure at 80°C to constant weight to obtain 5.8g of white crystalline powder. Example 3: Preparation method 3 of water-soluble daidzein

Embodiment 3

[0047] Take 5g of daidzein, add potassium hydroxide solution to dissolve, adjust the pH to 14, filter, add 100ml of acetone, stir evenly, leave it for 4 hours, filter, wash with a little acetone three times, and dry the precipitate at 40°C under reduced pressure. At constant weight, 4.4g of white crystalline powder is obtained. Example 4: Preparation method 4 of water-soluble daidzein

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Abstract

A water-soluble soybean aglucone is prepared from soybean glucone through dissolving the soybean glucone in the solution of inorganic and / or organic alkali, regulating pH to 9.5-14, stirring while adding low-carbon-chain unitary alcohol or ketone, stirring, laying aside for 1-4 hr, filtering, washing, depositing at 40-80 deg.c, and vacuum drying. Its advantages are high water solubility, absorbability, chemical stability and purity.

Description

Technical field [0001] The invention relates to a method for preparing water-soluble daidzein by using daidzein. This new compound can be used as a raw material for pharmaceutical preparations (solid dosage forms such as tablets, capsules, granules, dripping pills, etc.; liquid dosage forms such as powder injections, water injections, infusions, eye drops, oral liquids) Etc.) for the treatment of cardiovascular and cerebrovascular diseases; women's menopausal syndrome; osteoporosis and other diseases. It can be widely used in medicine, health products, food, beverage, cosmetics, animal medicine and other fields. Background technique [0002] Generic name: Daidzein [0003] Previous name: Pueraria lobata daidzein [0004] English name: Daidzein [0005] Chinese Pinyin: Huangdouganyuan [0006] Chemical name: 4′,7-dihydroxyisoflavone [0007] Chemical Structure: [0008] Molecular formula: C 15 H 10 O 4 [0009] Molecular weight: 254.24 [0010] Daidzein raw materials and their p...

Claims

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Application Information

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IPC IPC(8): A23L33/105A61K31/352A61P9/10A61P15/12A61P19/10C07D311/36
Inventor 于跃
Owner 沈阳海德医药化工有限公司