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Soy isoflavone solid dispersion suppository and preparation method thereof

A technology of soybean isoflavones and solid dispersions, applied in the field of medicine, can solve the problems of not being able to promote the conversion of glycoside aglycone, the effect is not very good, and the deglycoside aglycon is difficult to absorb.

Inactive Publication Date: 2010-06-02
SHANXI MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The purpose of methods (1) and (3) is to convert the inactive glycoside aglycone into highly active deglycoside aglycone, but it cannot solve the problem that the deglycoside aglycone is difficult to absorb; the second method It is to improve the water solubility of soybean isoflavones, but it cannot promote the transformation of glycoside aglycone
Therefore, none of the above three methods can fundamentally change the problem that free aglycon is difficult to absorb, and the effect is not very good.

Method used

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  • Soy isoflavone solid dispersion suppository and preparation method thereof
  • Soy isoflavone solid dispersion suppository and preparation method thereof
  • Soy isoflavone solid dispersion suppository and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0046] Embodiment 1, the preparation of soybean isoflavone vaginal suppository

[0047] 1) Preparation of soybean isoflavone solid dispersion by melting method

[0048] Weigh 5.0g of soybean isoflavones passed through a 80-mesh sieve and 10.0g of PEG4000 to co-melt on an 80°C water bath, stir for 1 hour, quickly place it in a -20°C freezer to cool for 4 hours, take it out and place it in a desiccator to balance for 48 hours, and crush it through 80 mesh Sieve to obtain a solid dispersion with a mass ratio of soybean isoflavones to PEG4000 of 1:2.

[0049] 2) Preparation of suppositories

[0050] The classic base gelatin of suppositories: glycerol: water = 7: 2: 1 is used as the base of soy isoflavone solid dispersion suppositories. Take 2.0g of gelatin and place it in an evaporating dish of known weight, add an appropriate amount of distilled water, soak for 30 minutes to soften the swelling, and drain the excess water. Add 7.0 g of glycerin and heat on a water bath to diss...

Embodiment 2

[0052] Embodiment 2, the preparation of soybean isoflavone vaginal suppository

[0053] 1) Preparation of soybean isoflavone solid dispersion by melting method

[0054] Weigh 5.0g of soybean isoflavone powder and 25.0g of PEG6000, mix evenly, pass through a 80 mesh sieve, place in an evaporating dish, heat it in a water bath to about 80°C to melt, stir vigorously, cool quickly in an ice-salt bath, and freeze for 3 hours , make it fully solidified, put it in a drier with a constant temperature of 40-50°C for 72 hours, grind it, pass through a 200-mesh sieve, and obtain a solid dispersion with a mass ratio of soybean isoflavones and PEG6000 of 1:5.

[0055] 2) Preparation of suppositories

[0056] Mix the soybean isoflavone solid dispersion prepared in step 1) with the glycerin gelatin matrix prepared in step 2) of Example 1 at a mass ratio of 1:10, stir evenly, heat to melt the above mixture, and inject the lubricant coated In the suppository mold, cool at room temperature, r...

Embodiment 3

[0057] Embodiment 3, the preparation of soybean isoflavone vaginal suppository

[0058] 1) Preparation of soybean isoflavone solid dispersion by melting method

[0059] Weigh 5.0g of soybean isoflavones passed through a 80 mesh sieve and 10.0g of PEG6000 to co-melt on an 80°C water bath, stir for 1 hour, quickly place it in a -20°C freezer to cool for 4 hours, take it out and place it in a desiccator to balance for 48 hours, and crush it through 80 mesh Sieve to obtain a solid dispersion with a mass ratio of soybean isoflavones and PEG6000 of 1:2.

[0060] 2) Preparation of suppositories

[0061] Mix the soybean isoflavone solid dispersion prepared in step 1) with the glycerin gelatin matrix prepared in step 2) of Example 1 at a mass ratio of 1:10, stir evenly, heat to melt the above mixture, and inject the lubricant coated In the suppository mold, cool at room temperature, remove the mold, absorb the water on the surface of the suppository with absorbent paper, and obtain t...

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Abstract

The invention discloses a soy isoflavone vaginal suppository and a preparation method thereof. Raw materials for preparing the suppository comprise soy isoflavone solid dispersion and a water-soluble substrate, wherein the soy isoflavone solid dispersion is prepared from soy isoflavone and a hydrophilic solid dispersion carrier, and the mass ratio of the soy isoflavone and the carrier is 1:1-20. The invention designs and prepares a soy isoflavone solid dispersion suppository for vaginal drug administration on the premise of overcoming the defect of poor absorption effect of the oral administration of the soy isoflavone. The solid dispersion technology improves the dispersity and the hydrophilism of the soy isoflavone and improves the moisture degree on the vagina mucosa, thereby improving the infiltration rate of the prepared suppository by 2-3 times. The suppository greatly improves the curative effect of the soy isoflavone on treating and mitigating a series of diseases of women caused by maladjustment of estrogen level.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a soybean isoflavone solid dispersion suppository and a preparation method thereof. Background technique [0002] In recent years, various diseases caused by menopausal women and young women caused by estrogen level imbalance are increasing year by year. Soy isoflavones, also known as "phytoestrogens", have a two-way regulating effect on estrogen levels in the human body, and are favored by women over 35 years old. At present, there are many soy isoflavone medicines, functional products and foods added with soy isoflavones in the market, but the curative effect of these products is not optimistic due to the poor oral absorption effect of soy isoflavones (absorption rate is only 13-30%). [0003] Soybean Isoflavone (English name: soybean Isoflavone) is a yellow or light yellow powder with a slightly bitter taste. Free type (glycon type) and glycoside type (including glucoside...

Claims

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Application Information

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IPC IPC(8): A61K9/02A61K31/352A61K47/42A61K47/40A61K47/38A61K47/34A61K47/32A61P5/30A61P15/02A61K47/10A61K47/14
Inventor 田青平王颖莉石恩娴杨波李菁徐珍
Owner SHANXI MEDICAL UNIV
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