WO2021093315A1

WO2021093315A1 - Composition for protecting liver, preparation method therefor, and application thereof

Info

Publication number: WO2021093315A1
Application number: PCT/CN2020/094510
Authority: WO
Inventors: 肖伟; 丁艳; 刘世娟; 王婧; 柏伟荣; 王振东; 邓辰辰
Original assignee: 江苏康仁医药科技开发有限公司
Priority date: 2019-11-12
Filing date: 2020-06-05
Publication date: 2021-05-20
Also published as: CN110934914A

Abstract

Disclosed is a composition for protecting liver, a preparation method therefor, and application thereof. The composition comprises Puerariae Lobatae Radix, Crataegi Fructus, Taraxaci Herba, Chrysanthemi Flos, and Citri Reticulatae Pericarpium.

Description

Composition with hepatoprotective function and preparation method and application thereof

Technical field

The invention relates to the technical fields of medicines, health products and foods, and in particular to a composition with liver protection function and a preparation method and application thereof.

Background technique

Drinking has a long history in our country, and the wine culture has penetrated into people's lives and work. However, long-term drinking can cause damage to the internal organs of the body and aggravate liver damage, because alcohol may cause the liver to accumulate more and more fat, which will gradually cause inflammation. When alcohol drinkers have symptoms of liver damage, often more than 3/4 of the liver cells have lost their normal function, which can cause liver fibrosis, cirrhosis and even primary liver cancer in severe cases. Therefore, it is of great significance to develop products that sober up and hangover, and reduce liver damage caused by alcohol with high safety.

Summary of the invention

One of the objectives of the present invention is to provide a composition with hepatoprotective function. The composition and the raw materials used can be directly ground into powder, or it can be an extract prepared by conventional means or other forms. The composition In terms of parts by weight, it includes: 150-300 parts of Pueraria lobata, 200-350 parts of hawthorn, 100-250 parts of dandelion, 100-200 parts of chrysanthemum, and 100-200 parts of tangerine peel.

In another embodiment of the present invention, the composition includes: 200-300 parts by weight of Pueraria lobata root, 200-300 parts of hawthorn, 100-200 parts of dandelion, 100-150 parts of chrysanthemum, and 100-150 parts of tangerine peel.

In another embodiment of the present invention, the composition includes 180-220 parts by weight of Pueraria lobata, 280-320 parts of hawthorn, 180-220 parts of dandelion, 140-160 parts of chrysanthemum, and 140-160 parts of tangerine peel.

In another embodiment of the present invention, the composition includes 200 parts by weight of Pueraria lobata, 300 parts of hawthorn, 200 parts of dandelion, 150 parts of chrysanthemum, and 150 parts of tangerine peel.

The present invention also proposes the application of any of the previous compositions in the preparation of medicines, health products or foods with hepatoprotective function. The liver protection function may be, for example, preventing or reducing liver damage caused by alcohol.

The present invention also proposes a medicine, health care product or food containing the composition with liver protection function as any one of the previous items.

In another specific embodiment of the present invention, the medicine, health product or food is selected from beverages, capsules, compressed candies, tablets, powders, teas, granules, oral liquids or granules.

In another specific embodiment of the present invention, the medicine, health product or food contains pharmaceutically or food-acceptable auxiliary materials or additives; for example, it may be erythritol, microcrystalline cellulose, strawberry fruit powder, maltodextrin, stevia Glycoside, magnesium stearate.

As a preferred embodiment, calculated in parts by weight, the acceptable excipients or additives include 1 to 3 parts of erythritol, 50 to 80 parts of microcrystalline cellulose, 10 to 15 parts of strawberry fruit powder, and 200 to 200 parts of maltodextrin. 300 parts, 0.5～1 steviol glycosides, 10～30 parts magnesium stearate.

In another alternative embodiment of the present invention, the medicine, health care product or food includes microcrystalline cellulose and maltodextrin; wherein, the microcrystalline cellulose is preferably 60 to 70 parts, and the maltodextrin is preferably 200 parts. ~300 copies.

The present invention also provides a method for preparing a health care product or food. When the health care product or food is selected from tableted candies, it is characterized in that the preparation method includes the following steps:

Weigh Pueraria lobata, hawthorn, dandelion, chrysanthemum, and tangerine peel in the aforementioned proportions, add 10-12 times of water, extract (optionally, the extraction time is 1h, the number of extractions is 2), and then concentrate at 60～70℃ (to a density of 1.1～ 1.2g/mL), dried, sieved after crushing;

Mix the sieved material with erythritol, strawberry fruit powder, maltodextrin, and steviol glycosides evenly, and the mixing time is optionally 20 min;

After the mixed powder is stirred, it is wet-granulated with alcohol and dried; the drying temperature is optionally 60°C, and the drying time is 50-70 minutes, until the moisture of the wet granules is below 5%;

Granulation and total mixing: the dried granules are granulated, and the mixed magnesium stearate and microcrystalline cellulose are mixed with the granular granules, and the mixing time is optionally 25-30 minutes;

Tableted to obtain tableted candies.

In another specific embodiment of the present invention, the preparation method of the compressed candy includes the following steps:

Take 200 parts of Pueraria lobata, 300 parts of hawthorn, 200 parts of dandelion, 150 parts of chrysanthemum, and 150 parts of tangerine peel, extract twice with 10 times water, concentrate at 65°C, dry in vacuum at 60°C, crush and pass through a 60-mesh sieve;

Put the sieved material and 10 parts of strawberry fruit powder, 1 part of erythritol, 250 parts of maltodextrin, and 0.5 part of steviol glycosides into the mixer, mix for 20 minutes, and mix well;

Granulation: The above mixed powder is made into soft material with 90% ethanol, and granulated with an 18-mesh sieve;

Drying: dry the wet granules at 60°C for 60 minutes;

Granulation and tableting: The dried granules are sized with a 20-mesh sieve, and then put into a mixer, and then magnesium stearate and microcrystalline cellulose powder are added in sequence, mixed, and the mixing time is 30 Minutes, tablet.

At present, there are few traditional Chinese medicine prescriptions that can protect the liver and regulate the liver. The present invention proposes a composition with liver-protecting function. Among the main raw materials, Pueraria lobata root has the functions of clearing the meridians, activating collaterals, relieving alcohol and toxins, producing body fluid and quenching thirst to quench thirst caused by alcohol, which belongs to the emperor's medicine. Hawthorn has the functions of eliminating the masses and strengthening the stomach, promoting qi and dispersing blood stasis, reducing turbidity and lowering lipids, and can achieve the purpose of promoting body fluids and quenching thirst; Chrysanthemum has the effects of calming the liver and improving eyesight, clearing away heat and detoxification, and the above three are the ministerial medicine. Tangerine peel has the function of regulating qi and invigorating the spleen and is an adjuvant. The above five herbs are shared to achieve the effects of producing body fluids and quenching thirst, regulating qi and eliminating pathogenic factors, and relieving alcohol and poison.

Not only that, the present invention also prepares tableted candies by adding auxiliary materials and process adjustment, adding fruit powder and flavoring agents to increase the pleasant taste of the product.

The tableted candy for relieving alcohol and protecting the liver provided by the present invention can achieve the effects of sobering up and relieving alcohol by accelerating the metabolism of alcohol, and it can also improve the abnormal metabolism caused by alcohol, regulate human body functions, and has the advantages of clearing heat and detoxification, producing body fluids and quenching thirst And the effect of invigorating the spleen and stomach and protecting the liver reduces the occurrence of alcoholic liver injury.

Detailed ways

The following describes the present invention in more detail through specific implementations, so as to better understand the solutions of the present invention and the advantages of various aspects thereof. However, the content of the specific embodiments described below is for illustrative purposes only, and is not a limitation to the present invention.

It should be noted that if the specific conditions are not specified, they will be carried out in accordance with the conventional conditions or the conditions recommended by the manufacturer. The raw materials or auxiliary materials used, and the reagents or instruments used without the manufacturer’s instructions are all commercially available. Regular products. Unless otherwise stated, all percentages, ratios, ratios or parts are by weight.

Unless otherwise defined, all professional and scientific terms used in the text have the same meaning as those familiar to those skilled in the art. In addition, any methods and materials similar or equivalent to the content described can be applied to the present invention.

Screening of auxiliary materials of the composition of the present invention

Take 200 parts of Pueraria lobata, 300 parts of hawthorn, 200 parts of dandelion, 150 parts of chrysanthemum, and 150 parts of tangerine peel, and extract twice with 10 times water. After extraction, it is concentrated at 65°C and dried in vacuum at 60°C. Crush it with 10 parts of strawberry fruit powder, 1 part of erythritol, microcrystalline cellulose and maltodextrin as shown in the table below, 0.5 parts of steviol glycosides and 10 parts of magnesium stearate into the mixer and mix for 20 minutes , After mixing uniformly, use 90% ethanol to make soft material, and use 18 mesh sieve for granulation.

Table 1 Selection of excipients and test results

Table 2 Selection of excipients and test results

It can be seen from the experimental results that when the amount of maltodextrin is 200-300 parts and the amount of microcrystalline cellulose is 60-70 parts, the product is not easy to agglomerate and is easy to sieving. Therefore, the weight parts of microcrystalline cellulose and malt are selected. Dextrin is the preferred excipient formula for this experiment.

Pharmacodynamic investigation of the composition of the present invention

1. Material

180 SPF-grade Wistar male rats, 180-220g, purchased from Beijing Weitong Lihua Laboratory Animal Technology Co., Ltd., license number: SCXK (京) 2016-0011. The animal experiment passed the animal ethics review of Beijing University of Traditional Chinese Medicine, and the number is: BUCM-4-2016120123-4023.

Anhydrous ethanol (Nanjing Chemical Reagent Co., Ltd., batch number 171225545K); AST kit (Nanjing Jiancheng Institute of Biological Engineering, batch number 20171024); ALT kit (Nanjing Jiancheng Institute of Biological Engineering, batch number 20171025); GSH reagent Kit (Nanjing Jiancheng Institute of Bioengineering, batch number 20171211); ADH kit (Nanjing Jiancheng Institute of Bioengineering, batch number 20171123); MDA kit (Nanjing Jiancheng Institute of Bioengineering, batch number 20171203).

2. Evaluation of acute toxicity

Take 40 rats, and divide them into groups (experimental group) and control group, 20 rats in each group. In the experimental group, rats were intragastrically administered with the sample prepared in Example 1 at 16 g (based on the amount of the preparation)/kg, and the administration volume was 40 ml/kg, 3 times a day for 15 days. The vehicle control group was treated with an equal volume of saline in the same way. Observe the rats' body weight changes, appearance, physical signs, behavioral activities, mental status, response to stimulation, secretions, excrement, and death within 15 days after administration. Preliminary pathological examinations were performed on the animals that died and the animals killed during the experiment. The tissues and organs of each animal were observed and recorded for abnormalities such as changes in volume, color, and texture.

Table 3 The effect of compressed candy on the body weight of rats during the experiment

General observation results The experimental drug group and the control group are in good mental state. The rats have no abnormal body size, normal behavior, brighter coat, normal breathing, no abnormal body size, eyes, skin, nose, nose, ears, etc. There was no abnormal secretion, redness, swelling, ulceration in the perineum, granular stool, and no death.

3. Hangover and liver protection experiment

Take 100 rats and randomly divide them into the high-dose group [18g/(kg·d)], the medium-dose group [9g/(kg·d)], and the high-dose group [18g/(kg·d)] according to their body weight. Jiubaogan compressed candy low-dose group [1.8g/(kg·d)] and model control group, each with 12 rats. Except for the model control group, each group was given the corresponding dose once a day by gavage, with a volume of 0.04 mL/g for 6 consecutive days. The control group was given an equal volume of saline in the same way. After 30 minutes of administration on the 6th day, each rat was intragastrically administered with 50% ethanol (diluted with water and absolute ethanol). After 1 hour, the eyeballs were removed to take blood, and the serum was separated. The activities of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in serum were determined according to the instructions of the kit. After the blood was collected, the cervical vertebrae were sacrificed, and the liver was weighed to prepare 10% liver homogenate. Determine the activity of glutathione (GSH), malondialdehyde (MDA) and alcohol dehydrogenase (ADH) in liver tissue according to the instructions of the kit.

Table 4 The effect of compressed candy on the activity of ALT and AST in serum

*P<0.05, **P<0.01.

The results in Table 4 show that compared with the model control group, both the middle and high dose groups can significantly reduce the ALT activity in rat serum (P＜0.05 or P＜0.01), and the low dose group also has a decreasing trend on the ALT activity in rat serum; The middle and high dose groups significantly inhibited the activity of AST in rat serum (P＜0.05 or P＜0.01), and the low dose group also had a tendency to decrease the AST in rat serum.

Table 5 The effect of compressed candy on the activity of GSH, MDA and ADH in liver tissue

*P<0.05, **P<0.01.

The results in Table 5 show that, compared with the model control group, both the middle-dose group and the high-dose group can significantly reduce the activity of MDA in rat liver tissue (P<0.05), and significantly increase the activity of GSH and ADH in liver tissue (P<0.05 or P<0.01), the low-dose group can also reduce GSH in liver tissue to a certain extent, or increase the activity of GSH and ADH in liver tissue.

It can be seen from the above that the composition of the present invention can increase the activity of GSH and ADH in liver tissue and reduce the activity of ALT and AST in serum, indicating that it has obvious anti-alcohol and liver-protecting effects.

Example 1

Take 200 parts of Pueraria lobata, 300 parts of hawthorn, 200 parts of dandelion, 150 parts of chrysanthemum, and 150 parts of tangerine peel, and extract twice with 10 times water. After extraction, it is concentrated at 65°C and dried in vacuum at 60°C. Crush, put 10 parts of strawberry fruit powder, 1 part of erythritol, 250 parts of maltodextrin, and 0.5 part of steviol glycosides into a mixer, mix for 20 minutes, and granulate after mixing.

Granulation: The above-mentioned mixed powder is made into a soft material with 90% ethanol, and granulated with an 18-mesh sieve.

Drying: Put the wet granules on the drying bed, the inlet air temperature is 60℃, and dry for 60min.

Granulation and tableting: use a 20-mesh sieve to sizing the dried granules, put them in a mixer, add 10 parts of magnesium stearate and 70 parts of fine microcrystalline cellulose powder, mix, and mix time For 30 minutes. The qualified granules are added to the material container of the tablet press for tablet compression. In this example, a total of 1000 parts of medicinal materials are used to obtain 241.5 parts of tableted candies, each of which is about 0.35 to 0.4 g.

Example 2

Take 300 parts of Pueraria lobata, 300 parts of hawthorn, 150 parts of dandelion, 100 parts of chrysanthemum, and 150 parts of dried tangerine peel, extract twice with 10 times water, concentrate at 60°C after extraction, and dry at 80°C in vacuum. Crush it, put 15 parts of strawberry fruit powder, 2 parts of erythritol, 200 parts of maltodextrin, and 0.5 part of stevioside into a mixer, mix for 20 minutes, and then granulate after mixing.

Granulation and tableting: The dried granules are sized with a 20-mesh sieve, and then placed in a mixer, and then 10 parts of magnesium stearate and 60 parts of microcrystalline cellulose are added, and the mixing time is 30 minute. The qualified granules are added to the material container of the tablet press for tablet compression. In this example, a total of 1000 parts of medicinal materials are used to obtain 241.5 parts of tableted candies, and each tablet is about 0.35 to 0.40 g.

The description of the above embodiments is only used to help understand the method and core idea of the present invention. It should be pointed out that for those of ordinary skill in the art, without departing from the principle of the present invention, several improvements and modifications can be made to the present invention, and these improvements and modifications also fall within the protection scope of the claims of the present invention.

Claims

A composition with hepatoprotective function, characterized in that, calculated in parts by weight, the composition comprises: 150-300 parts of pueraria, 200-350 parts of hawthorn, 100-250 parts of dandelion, 100-200 parts of chrysanthemum, and dried tangerine peel 100 to 200 copies.
The composition according to claim 1, characterized in that the composition, calculated in parts by weight, comprises: 200-300 parts of Pueraria lobata, 200-300 parts of hawthorn, 100-200 parts of dandelion, 100-150 parts of chrysanthemum, dried tangerine peel 100 to 150 copies.
The composition according to claim 1, wherein the composition, calculated in parts by weight, comprises: 180-220 parts of Pueraria lobata, 280-320 parts of hawthorn, 180-220 parts of dandelion, 140-160 parts of chrysanthemum, dried tangerine peel 140 to 160 copies.
The composition according to claim 1, wherein the composition comprises 200 parts by weight of Pueraria lobata, 300 parts of hawthorn, 200 parts of dandelion, 150 parts of chrysanthemum, and 150 parts of tangerine peel.
The use of the composition of any one of claims 1 to 4 in the preparation of medicines, health products or foods with hepatoprotective function.
A medicine, health care product or food containing a composition with liver protection function according to any one of claims 1-4.
The medicine, health product or food according to claim 6, wherein the medicine, health product or food is selected from the group consisting of beverages, capsules, compressed candies, tablets, powders, teas, granules, oral liquids or granules Agent.
The medicine, health product or food according to claim 6, wherein the medicine, health product or food comprises microcrystalline cellulose and maltodextrin; wherein the microcrystalline cellulose is preferably 60-70 parts, The maltodextrin is preferably 200-300 parts.
A method for preparing the health care product or food according to claim 6, when the health care product or food is selected from tableted candies, it is characterized in that the preparation method comprises the following steps:

Weigh Pueraria lobata, hawthorn, dandelion, chrysanthemum, tangerine peel, add 10-12 times of water, extract, concentrate at 60-70°C, dry, crush and sieving;

Mix the sieved material with erythritol, strawberry fruit powder, maltodextrin and steviol glycosides;

After the mixed powder is stirred, it is wet-granulated with alcohol and then dried;

Granulation and total mixing: the dried granules are granulated, and the mixed magnesium stearate and microcrystalline cellulose are mixed with the granular granules;

Tableted to obtain tableted candies.
A method for preparing the health care product or food according to claim 6, when the health care product or food is selected from tableted candies, it is characterized in that the preparation method comprises the following steps:

Take 200 parts of Pueraria lobata, 300 parts of hawthorn, 200 parts of dandelion, 150 parts of chrysanthemum, and 150 parts of tangerine peel, extract twice with 10 times water, concentrate at 65°C, dry in vacuum at 60°C, crush and pass through a 60-mesh sieve;

Put the sieved material and 10 parts of strawberry fruit powder, 1 part of erythritol, 250 parts of maltodextrin, 0.5 part of steviol glycosides into the mixer, and mix for 20 minutes, and mix evenly;

Granulation: The above mixed powder is made into soft material with 90% ethanol, and granulated with an 18-mesh sieve;

Drying: dry the wet granules at 60°C for 60 minutes;

Granulation and tableting: The dried granules are sized with a 20-mesh sieve, and then put into a mixer, and then 10 parts of magnesium stearate and 70 parts of microcrystalline cellulose are added in sequence, mixed, and mixing time Compress the tablet for 30 minutes.