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Genistein clathrate compound-containing preparation and its preparation method and use

A technology of genistein and clathrate, applied in the field of medicine, can solve the problems of increasing the risk of adverse reactions, limiting the types of preparations, increasing the cost of medication, etc., and achieving easy industrial production, rapid curative effect, economical and social High benefit effect

Inactive Publication Date: 2012-01-18
李荣立
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Genistein is almost insoluble in water, and its poor water solubility makes it difficult for the preparations prepared by traditional preparation methods to achieve the bioavailability required for treating diseases after oral administration, which also greatly limits the production of preparations. Type, such as dosage forms such as soluble powders or intravenous formulations
In addition, the content of genistein in the preparation is low, and in order to achieve the therapeutic drug concentration, the curative effect can only be improved by increasing the dosage of the preparation, but this increases the risk of adverse reactions to a certain extent, It also increases the cost of medication

Method used

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  • Genistein clathrate compound-containing preparation and its preparation method and use
  • Genistein clathrate compound-containing preparation and its preparation method and use
  • Genistein clathrate compound-containing preparation and its preparation method and use

Examples

Experimental program
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Effect test

Embodiment 1

[0108] Example 1: Preparation of genistein freeze-dried powder for injection

[0109] Weigh 2.0g of genistein, 60.0g of hydroxypropyl-β-cyclodextrin, and 124g of mannitol, first dissolve genistein in 130ml of ethanol, stir to dissolve, then add hydroxypropyl-β-cyclodextrin Refining, magnetic stirring for 2 hours, temperature 50°C, after clathrate, remove ethanol under reduced pressure, add mannitol and water for injection 1000ml and stir to dissolve, add water for injection to 2000ml full amount, adjust pH to 3.3 with citric acid, add drug Stir and adsorb with activated carbon for 15 minutes, the amount of medicinal carbon used is 0.03%, filter, the filtrate is divided into vials, freeze-dried, vacuum-pressed and taken out, and the aluminum-pressed cap is labeled to obtain the freeze-dried product.

Embodiment 2

[0110] Embodiment 2: Preparation of Genistein Sodium Chloride Injection

[0111]Weigh 40.0g of hydroxypropyl-β-cyclodextrin, 1.0g of genistein and 9.0g of sodium chloride for injection, add genistein to 60ml of ethanol, stir to dissolve and add hydroxypropyl -β-cyclodextrin and sodium chloride for injection, magnetically stirred for 1 hour (control the speed so that the liquid does not splash outwards), temperature 60°C, observed to obtain clear and transparent genistein hydroxypropyl-β-cyclodextrin clathrate solution. Remove ethanol under reduced pressure, add water for injection to 600ml and stir, add water for injection to 1000ml full amount, adjust pH to 3.8 with tartaric acid, add medicinal active carbon and stir for adsorption for 20 minutes, the amount of medicinal carbon used is 0.03%, filter, press The predetermined dose is divided into infusion bottles and sterilized by autoclaving at 115°C for 30 minutes.

Embodiment 3

[0112] Embodiment 3: Preparation of Genistein Glucose Injection

[0113] Weigh 50.0g of hydroxypropyl-β-cyclodextrin, 2.0g of genistein, and 50g of glucose for injection, add genistein to 150ml of ethanol, stir and dissolve, then add hydroxypropyl-β- Cyclodextrin, stirred by magnetic force for 1 hour (the speed is controlled so that the liquid does not splash outside), the temperature is 55° C., and a clear and transparent genistein hydroxypropyl-β-cyclodextrin inclusion complex solution is obtained. Ethanol was removed under reduced pressure. After glucose for injection and 100ml of water for injection are stirred and dissolved, the glucose solution is poured into the clathrate, replenished to 800ml, adjusted to pH 3.8 with tartaric acid, added with medicinal activated carbon and stirred and adsorbed for 20 minutes. The amount of medicinal carbon used is 0.03%, filtered, divided into infusion bottles according to the predetermined dose, and sterilized at 115°C for 30 minutes...

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Abstract

The invention discloses a genistein clathrate compound, a genistein clathrate compound-containing preparation and a preparation method of the genistein clathrate compound-containing preparation. A preferred clathrating agent adopted by the preparation method is cyclodextrin or a cyclodextrin derivative. The genistein clathrate compound comprises: by weight, 1-100 parts of genistein and 5-800 parts of cyclodextrin or a cyclodextrin derivative. Through clathration effects of cyclodextrin or a cyclodextrin derivative on genistein, the water-solubility of genistein is improved. The genistein clathrate compound can be further prepared into different dosage forms suitable for clinical use, and can improve greatly the bioavailability of genistein. The genistein clathrate compound and the genistein clathrate compound-containing preparation have good effects of preventing and treating osteoporosis, female menopause syndrome, tumor, cardio-cerebrovascular diseases and the like.

Description

technical field [0001] The present invention relates to a pharmaceutical composition and its preparation. Specifically, the present invention relates to a genistein inclusion compound, a preparation containing genistein inclusion compound and its preparation method and use, belonging to the pharmaceutical field. Background technique [0002] Genistein is soluble in DMSO and ethanol, almost insoluble in water, the structure is as follows: [0003] [0004] Genistein is an isoflavone compound derived from legumes and dentate plants, and its chemical name is 4',5,7-trihydroxyisoflavone. It is the main active ingredient of soybean isoflavones, which has estrogen-like effects in the metabolism in the body, and is called phytoestrogens. Genistein has a variety of pharmacological effects and biological activities such as preventing early atherosclerosis and chronic vascular diseases, anti-tumor, and women's climacteric syndrome. Genistein is a powerful inhibitor of tyrosine p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/352A61P35/00A61P19/10A61P15/12A61P9/00
Inventor 李荣立赵素芬
Owner 李荣立
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