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Method for preparing soybean isoflavone sustained-release microspheres

A technology of soybean isoflavones and sustained-release microspheres, which is applied in the directions of non-active ingredients medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc. The effect of prolonged release time and excellent sustained release performance

Inactive Publication Date: 2013-08-21
THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no corresponding report on making long-acting sustained-release preparations of soybean isoflavones such as genistein. Compared with common preparations, the sustained-release preparations made of soybean isoflavones can release medicine slowly, and the dosing frequency can be increased. decreased, and can significantly increase the efficacy of the drug

Method used

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  • Method for preparing soybean isoflavone sustained-release microspheres
  • Method for preparing soybean isoflavone sustained-release microspheres

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preparation example Construction

[0015] A preparation method of soybean isoflavone sustained-release microspheres, comprising the steps of:

[0016] (1) Dissolve 0.3-2.5g of polyvinyl alcohol (PVA) in 30-50ml of double-distilled water to make a double-distilled water solution of polyvinyl alcohol;

[0017] (2) Add 0.03-0.1g of soybean isoflavones and 0.3-1.0g of PLGA into 10ml of dichloromethane, mix and ultrasonically emulsify at room temperature for 5-15 minutes;

[0018] (3) At a stirring speed of 800r / min, add the mixed solution obtained after ultrasonic emulsification in step (2) into the polyvinyl alcohol double distilled aqueous solution dropwise, stir for 5-15min, then adjust the stirring speed to 300r / min, continue to stir for 3 to 5 hours until the dichloromethane is completely volatilized;

[0019] (4) Centrifuge the mixture obtained in step (3) in a centrifuge at a temperature of 4°C and a rotation speed of 3000r / min for 5 minutes. After centrifugation, the upper layer of the mixture is liquid, ...

Embodiment 1

[0023] Weigh 0.6g of PVA with a molecular weight between 7000 and 14000, and dissolve it in 30ml double-distilled water to make a double-distilled solution of polyvinyl alcohol; weigh 0.05g of soybean isoflavones and 0.5g PLGA between them, the two were added in 10ml of dichloromethane, and ultrasonic 10min at room temperature, so that soybean isoflavones and PLGA were fully dissolved in dichloromethane; then at a stirring speed of 800r / min, the Add the mixed solution of soy isoflavones, PLGA and dichloromethane after ultrasonication into the polyvinyl alcohol double-distilled aqueous solution, stir for 10 minutes, adjust the stirring speed to 300r / min, and continue stirring for 5 hours until the dichloromethane is completely volatilized; Then the above-mentioned mixture without dichloromethane was centrifuged in a centrifuge with a temperature of 4°C and a rotation speed of 3000r / min for 5min. After centrifugation, the upper layer of the mixture was liquid, and the lower layer...

Embodiment 2

[0025] Weigh 0.8g of PVA with a molecular weight between 7000 and 14000, and dissolve it in 40ml of double distilled water to make a double distilled water solution of polyvinyl alcohol; weigh 0.05g of soybean isoflavones and 0.5g PLGA between them, the two were added in 10ml of dichloromethane, and ultrasonic 10min at room temperature, so that soybean isoflavones and PLGA were fully dissolved in dichloromethane; then at a stirring speed of 800r / min, the Add the mixed solution of soy isoflavones, PLGA and dichloromethane after ultrasonication into the polyvinyl alcohol double-distilled aqueous solution, stir for 10 minutes, adjust the stirring speed to 300r / min, and continue stirring for 5 hours until the dichloromethane is completely volatilized; Then the above-mentioned mixture without dichloromethane was centrifuged in a centrifuge with a temperature of 4°C and a rotation speed of 3000r / min for 5min. After centrifugation, the upper layer of the mixture was liquid, and the lo...

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Abstract

The invention discloses a method for preparing soybean isoflavone sustained-release microspheres, and relates to a method for preparing a medicinal sustained-release preparation. The method comprises the following steps of: preparing a polyvinyl alcohol double-distilled aqueous solution with certain concentration, performing ultrasonic emulsification on soybean isoflavone and polylactic-co-glycolic acid (PLGA) in a weight ratio of 1:15-1:5 in dichloromethane for certain time at normal temperature, dripping the ultrasonic mixed solution into the polyvinyl alcohol double-distilled aqueous solution, stirring till the dichloromethane is completely volatilized, performing centrifugal separation on the obtained mixed solution, and thus obtaining the soybean isoflavone sustained-release microspheres. The soybean isoflavone sustained-release microspheres prepared by using the PLGA as a matrix material have excellent sustained-release performance, and the release time of the microspheres in vitro is prolonged; and the sustained-release period of the prepared genistein sustained-release microspheres can reach 30 days, the microspheres have smooth surfaces and are round and non-sticky, the particle diameter can be controlled, the drug loading capacity is over 7 percent, and the encapsulated ratio is over 60 percent.

Description

technical field [0001] The invention relates to a preparation method of a drug sustained-release preparation, in particular to a preparation method of soybean isoflavone sustained-release microspheres. Background technique [0002] Soy isoflavones are a kind of phytochemicals, belonging to plant flavonoids, mainly derived from the pods of legumes. It is a mixture of polyphenols, which contains various components, mainly daidzein, genistein, soybean yellow genistin, daidzin and other substances. Soy isoflavone is a natural plant health product, and has many medicinal functions. In recent years, soybean isoflavones have been hot at home and abroad, and soy isoflavone health products, pharmaceutical tablets, oral liquids, etc. have been researched one after another. functional product. The main components thereof, such as genistein (GEN), also known as genistein, clinical studies have shown that it has a good preventive effect on breast cancer, prostate cancer, cardiovascular...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/352A61K47/32A61K47/34A61P9/00A61P15/12A61P35/00
Inventor 冯笑山张广平韩丹
Owner THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF SCI & TECH