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Preparation method of soybean isoflavone-chitosan slow-release microcapsules

A technology of soybean isoflavones and chitosan, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of low absorption rate, complicated operation, limited effect, etc. The effect of stable quality, uniform particles and high production efficiency

Active Publication Date: 2013-05-15
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are many commercially available SI soft capsules, the actual effect is limited. This is mainly because SI is a fat-soluble drug with low absorption rate in the body, low blood drug concentration, and fast metabolic degradation, resulting in insignificant drug effects. This largely limits the application of SI
[0003] In recent years, chitosan has been widely used as a controlled and sustained release material in oral drug delivery systems. Soy isoflavone sustained release microcapsules have been prepared using chitosan, sodium alginate or other materials alone as wall materials at home and abroad. However, due to the shortcomings of microcapsule drug loading and low encapsulation efficiency, it affects the pharmacodynamic effect of soybean isoflavones.
Moreover, the traditional preparation process is complex in operation, poor in controllability, and cannot be automated and industrialized on a large scale. Therefore, there is no soy isoflavone sustained-release preparation on the market at present.

Method used

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  • Preparation method of soybean isoflavone-chitosan slow-release microcapsules
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  • Preparation method of soybean isoflavone-chitosan slow-release microcapsules

Examples

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preparation example Construction

[0023] The preparation method of soybean isoflavone-chitosan sustained-release microcapsules comprises the following steps:

[0024] 1) prepare A liquid, A liquid is the calcium chloride chitosan gel liquid containing acetic acid, calcium chloride, chitosan, calcium chloride, chitosan, acetic acid are fully dissolved in distilled water successively during preparation;

[0025] 2) To prepare liquid B, mix the mixed sol solution containing sodium alginate with a mass concentration of 1%-3% and the mass-volume concentration of 10mg / ml-40mg / ml soybean isoflavones, and stir the mixed sol solution evenly with a stirrer Get liquid B;

[0026] 3) Gelation reaction, drop liquid B into liquid A by means of centrifugal granulation, trigger gelation reaction of liquid B, and generate soybean isoflavone-chitosan sustained-release microcapsules.

Embodiment 1

[0028] 1. Preparation of liquid A: First, pour 2L of single distilled water into a large beaker, and use a magnetic stirrer to fully dissolve in the order of anhydrous calcium chloride (20g), chitosan (10g), and acetic acid (20mL) in 2L single distilled water (dissolve calcium chloride fully first, then add chitosan to fully dissolve).

[0029] 2. Prepare liquid B: first pour 2L of single distilled water into a large beaker, then weigh 30g of sodium alginate, and dissolve it in 2L of single distilled water. The dissolution process needs to be heated in a water bath, and the temperature is controlled within the range of 60°C to 70°C. During the heating process, it should be fully stirred and emulsified until there are no granular particles and bubbles in the solution; measure 500mL of sodium alginate solution and pour it into a beaker, add 15g of soybean isoflavones that have been weighed, and stir well with a glass rod , until there are no small drug particles in the solution...

Embodiment 2

[0036] The difference from Example 1 is that when preparing liquid B, the selected concentration of sodium alginate is 1.00%: the relative yield of the obtained soybean isoflavone-chitosan sustained-release microcapsules is 79.5%, and the encapsulation efficiency is 62.5% , the drug loading was 23.6%.

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Abstract

The invention provides a preparation method of soybean isoflavone-chitosan slow-release microcapsules and relates to a method for preparing slow-release microcapsules. At present, microcapsule drug loading capacity and encapsulation efficiency are low, a pharmacodynamic effect of soybean isoflavone is influenced, operation is complex, controllability is poor, and mass production can not be achieved. The preparation method comprises the following steps of: preparing a solution A, wherein the solution A is calcium chloride chitosan gel containing acetic acid, calcium chloride and chitosan; preparing a solution B, namely uniformly dispersing a mixed sol solution containing sodium alginate with the mass concentration of 1-2% and soybean isoflavone with the mass-volume concentration of 10-40mg / ml by stirring by a stirrer, so as to obtain the solution B; and carrying out a gelation reaction, namely dropping the solution B into the solution A in a centrifugal pelletizing manner to initiate the gelation reaction, so as to generate the microcapsules. By adopting the preparation method provided by the invention, production efficiency is high; quality is stable, particles are uniform, and relative productivity is high; drug loading capacity is above 30%; encapsulation efficiency is more than 60%; and accumulation release rate for 4 hours is less than 40%.

Description

technical field [0001] The invention relates to a method for preparing sustained-release microcapsules. Background technique [0002] Humans have been eating soybeans for thousands of years. Soy isoflavone (Soy Isoflavone, SI) is a biologically active substance extracted from the natural plant soybean. A large number of experiments and clinical studies at home and abroad have found that SI has a wide range of pharmacological effects such as regulating blood lipids, preventing and treating cancer, anti-aging, improving women's climacteric syndrome, and improving osteoporosis. Cholesterol (TC), total triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), and increase high-density lipoprotein cholesterol (HDL-C), have the effects of regulating blood lipids and anti-atherosclerosis. Although there are many commercially available SI soft capsules, the actual effect is limited. This is mainly because SI is a fat-soluble drug with low absorption rate in the body, low blo...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/352A61K47/36A61P3/06A61P9/10
Inventor 窦晓兵胡林峰高佳陈宣光
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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