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Preparation method of nattokinase microcapsules

A technology of nattokinase and plant polyphenols, applied in biochemical equipment and methods, microcapsules, medical preparations of non-active ingredients, etc., can solve the problems of unstable microcapsules and low encapsulation efficiency of nattokinase, Achieve the effect of improving bioavailability, improving stability and improving encapsulation efficiency

Active Publication Date: 2020-04-17
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problems of low encapsulation efficiency and unstable microcapsules of existing nattokinase, the present invention provides a preparation method of novel nattokinase microcapsules, in which nattokinase is finally encapsulated by plant polyphenolic fatty acid ester , to ensure high stability of nattokinase microcapsule enzyme activity and long storage time, so that nattokinase can overcome the first-pass effect, increase the absorption of nattokinase in the small intestine, improve its antithrombotic effect, and greatly improve the bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Step 1) Take 2 g of burnet, 3.2 g of 3-methyl fatty acid chloride, 4.8 g of sodium hydroxide, and 20 mL of dioxane, and react at 100° C. for 3 h under nitrogen protection. The product is dissolved in petroleum ether and washed with saturated brine. The petroleum ether was distilled off under reduced pressure to obtain the burnet-(3)-methyl fatty acid chloride complex, which can be dried and stored.

[0026] Step 2), according to the mass ratio of burletin-(3)-methyl fatty acid chloride complex, isopropyl myristate, nattokinase freeze-dried powder and water is 1:20:2:77, take step 1 3 g of the obtained product, 60 g of isopropyl myristate, 6 g of lyophilized nattokinase powder and 231 g of water were mixed and homogenized by an ultrasonic cell disruptor for 1 min to obtain a W / O emulsion embedding nattokinase.

[0027] Step 3), take 100mL of the emulsion and add it to the feeder of the molecular distillation equipment. In the high vacuum distillation method, the distilla...

Embodiment 2

[0029] Step 1), take 2g of cinnamon polyphenols, 4g of hexanoyl chloride, 4g of sodium hydroxide, and 20mL of dioxane, and react at 100°C for 4h under nitrogen protection. The product is dissolved in petroleum ether and washed with saturated brine, and the petroleum ether is removed by distillation under reduced pressure. The obtained cinnamon polyphenol-caproyl chloride complex can be dried and stored.

[0030] Step 2), according to the mass ratio of cinnamon polyphenol-caproyl chloride complex, triglyceride, nattokinase freeze-dried powder and water is 2:25:3:70, take the product obtained in step 1 6g, triglyceride 60 g, 9 g of nattokinase freeze-dried powder and 210 g of water were mixed and then homogenized by an ultrasonic cell disruptor for 1 min to obtain a W / O emulsion embedding nattokinase.

[0031] Step 3), take 100mL of the emulsion and add it to the feeder of the molecular distillation equipment. In the high vacuum distillation method, the distillation temperature ...

Embodiment 3

[0033] Step 1), take 1g of aloe-emodin, 3g of octanoyl chloride, 3.5g of sodium hydroxide, and 20mL of dioxane, react for 5h at 100°C under nitrogen protection, dissolve the product in petroleum ether and wash with saturated brine, and distill off the petroleum under reduced pressure Ether to obtain the emodin-octanoyl chloride complex, which can be dried and stored.

[0034] Step 2), according to the mass ratio of emodin-octanoyl chloride complex, corn oil, nattokinase lyophilized powder and water is 3:30:2:67, take 9g of the product obtained in step 1, 90g of triglyceride, sodium After mixing 6 g of soybean kinase freeze-dried powder and 201 g of water, it was homogenized by an ultrasonic cell disruptor for 1 min to obtain a W / O emulsion embedding nattokinase.

[0035] Step 3), take 100mL of the emulsion and add it to the feeder of the molecular distillation equipment. In the high vacuum distillation method, the distillation temperature is 80°C, the condensation surface temp...

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Abstract

The invention discloses a preparation method of nattokinase microcapsules. The method comprises the following steps: mixing plant polyphenol and fatty acyl chloride, dissolving the plant polyphenol and fatty acyl chloride in dioxane, and making a reaction at a temperature of 100 DEG C for 3-5 hours under the action of an alkaline substance and the protection of nitrogen to obtain a reaction product, and carrying out after-treatment to obtain plant polyphenol fatty acid ester; taking 2-5wt% of nattokinase freeze-dried powder, 20-35wt% of oi phase, 1-5wt% of plant polyphenol fatty acid ester, and 60-80wt% of water phase based on the 100% of total mass fraction, mixing the materials, performing homogenizing by an ultrasonic cell disruptor to obtain a W / O type emulsion embedded with the nattokinase, adding the emulsion in a feeder of molecular distillation equipment and carrying out high-vacuum distillation for 15 to 30min under the pressure of 100-180 Pa at a distillation temperature of 50-100 DEG C and a condensation surface temperature of 20-30 DEG C and at a feed liquid flow rate of 4-10 mL / min, thereby obtaining nattokinase microcapsules having plant polyphenol coated with nattokinase. With the preparation method, the encapsulation efficiency of nattokinase can be greatly improved and the stability of the nattokinase microcapsules can be improved, so that the bioavailability of the nattokinase microcapsules is improved in a disguised manner.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical dosage forms, and relates to a preparation method of microcapsules, in particular to a preparation method of novel nattokinase microcapsules. Background technique [0002] Nattokinase (nattolinase, NK) was first discovered and named by Japanese scientist Dr. Sumi Yoko in 1987. It is a serine protease with strong fibrinolytic activity extracted from natto, a traditional Japanese fermented food. Nattokinase is an alkaline protease, composed of 275 amino acids, with a molecular weight of about 28kDa, and its sequence is similar to that of Bacillus subtilisin. Nattokinase can directly dissolve fibrin, and thrombus is formed by the accumulation of platelets and fibrin. Nattokinase can dissolve fibrin, and then it can prevent and treat thrombosis and related diseases, such as coronary heart disease, angina pectoris and stroke. Therapeutic effect. Nattokinase is relatively stable when the temper...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K38/48A61K47/14A61P7/02
CPCA61K9/5015A61K38/482A61P7/02C12Y304/21062
Inventor 王培鑫翟晚娜王纯洁金志敏
Owner ZHEJIANG UNIV OF TECH