JP7142857B2 - Carbohydrate absorption inhibitor - Google Patents

Description

TECHNICAL FIELD The present invention relates to a carbohydrate absorption inhibitor, and more particularly to a carbohydrate absorption inhibitor containing pu-erh tea as an active ingredient, wherein the pu-erh tea is raw tea.

Carbohydrates include those that are digested and absorbed by the body (sugar) and those that are not (dietary fiber). Carbohydrates are contained as starch not only in sweet foods such as sugar and fruits, but also in rice, bread, noodles, potatoes and the like.

BACKGROUND ART In recent years, various lifestyle-related diseases, which are thought to be caused by overnutrition and the like, are increasing. Many of these lifestyle-related diseases are triggered by excessive intake of carbohydrates, and examples thereof include diabetes and obesity. When starch is ingested, it is first degraded into α-dextrin by salivary amylase, then from the stomach to the duodenum, maltodextrin by α-amylase, and then hydrolyzed into the disaccharides maltose and isomaltose. be. On the other hand, sucrose, which is a disaccharide, reaches the small intestine without being decomposed in the digestive organs. These disaccharides are decomposed into monosaccharides, which are constituent sugars, by α-glucosidase, a membrane enzyme localized in the microvilli of the small intestine, and the decomposed monosaccharides are absorbed from the epithelial membrane of the small intestine. Absorbed monosaccharides enter the capillaries within the epithelial cells of the small intestine and are sent to the liver through the portal vein.

When carbohydrates such as starch and sucrose are ingested, they are absorbed from the small intestine and the blood sugar level (blood glucose concentration) rises sharply. Normally, when the blood sugar level rises, the secretion of insulin from the pancreas is stimulated, and the insulin concentration in the blood increases. Insulin lowers the blood sugar level by acting on glucose transporters that exist mainly in adipose tissue and skeletal muscle, and taking in blood glucose from there.

When excess carbohydrates are ingested, some of the glucose absorbed from the small intestine is stored as glycogen in the liver and skeletal muscle, but there is a limit to this amount, and the excess glucose is taken up by fat cells. Excessive carbohydrate intake causes obesity because it accumulates in adipose tissue.

Also, if you take too much sugar, the amount of glucose that must be processed increases in the blood, so the amount of insulin secreted from the pancreas increases. , the function deteriorates. When pancreatic function declines, insulin secretion declines, making diabetes more likely to occur. Excessive blood sugar damages blood vessels, leading to diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, and the like.

In addition, obesity tends to cause insulin resistance, in which insulin does not work normally in the liver, muscle, fat cells, and the like. Insulin resistance increases the need for insulin, which also causes pancreatic dysfunction. In addition, when insulin resistance occurs, VLDL (very low density lipoprotein) containing a large amount of triglycerides is excessively released from the liver into the blood, and LPL (lipoprotein lipase) is not sufficiently activated. , VLDL is less likely to be metabolized into HDL (high-density lipoprotein), and HDL cholesterol in the blood is lowered, making hyperlipidemia more likely. Hyperlipidemia causes arteriosclerosis.

Hyperglycemia caused by excessive intake of carbohydrates, that is, as a treatment for diabetes, insulin therapy that compensates for insufficient insulin from outside the body and lowers blood sugar levels, promotes insulin secretion, and improves insulin resistance Oral hypoglycemic drugs such as

Japanese Unexamined Patent Application Publication No. 2005-21025

Insulin therapy and oral hypoglycemic drugs that promote insulin secretion and improve insulin resistance increase body weight and body fat because insulin causes excess blood sugar in the blood to be taken into adipose tissue. However, obesity and hyperlipidemia may progress easily.

Therefore, in the first place, it is effective to suppress the absorption of carbohydrates in the digestive organs in order to suppress various diseases caused by excessive intake of carbohydrates. That is, an object of the present invention is to provide a novel carbohydrate absorption inhibitor that suppresses absorption of carbohydrates in the digestive organs.

As a result of intensive studies by the present inventors, the inventors have found that raw pu-erh tea has an excellent effect of suppressing carbohydrate absorption in the digestive organs, and have completed the present invention.

That is, the present invention provides a carbohydrate absorption inhibitor containing pu-erh tea as an active ingredient, wherein the pu-erh tea is raw tea.
Since the carbohydrate absorption inhibitor of the present invention exerts an excellent carbohydrate absorption inhibitory action in the digestive organs, it can suppress an excessive rise in blood sugar, and can prevent damage to blood vessels and exhaustion of the pancreas. can be suppressed. In addition, diabetes, hyperglycemia, obesity, hyperlipidemia, arteriosclerosis, etc. can be prevented, alleviated or treated by the carbohydrate absorption inhibitory action.

Moreover, the carbohydrate absorption inhibitor may be for oral administration or ingestion. Raw pu-erh tea has been ingested as a beverage since ancient times, and oral safety has been established. A patient or consumer convenient method of ingestion is available. In addition, oral administration or ingestion enhances the effect as a carbohydrate absorption inhibitor.

Moreover, the carbohydrate absorption inhibitor may be in the form of an aerosol, liquid, capsule, granule, pill, powder, tablet, or syrup. By being in the above form, it is easier for patients or consumers to administer or take, and it is also advantageous in terms of preservation/storage and distribution.

INDUSTRIAL APPLICABILITY According to the present invention, a novel carbohydrate absorption inhibitor is provided that exerts an excellent carbohydrate absorption inhibitory action in the digestive organs.

Fig. 2 shows changes in portal vein blood glucose concentration of rats to which (a) raw tea sample or (b) ripe tea sample was orally administered, measured by the carbohydrate absorption inhibition test of the example of the present application. In the figure, the error bars indicate the mean ± standard error, "*" p-value is less than 5%, "**" p-value is less than 1%, in portal vein plasma before sample administration (0 min) It shows that there is a significant difference compared to the glucose concentration values.

(Pu-erh tea)
The carbohydrate absorption inhibitor of the present invention contains raw Pu-erh tea as an active ingredient. Hereinafter, the term "raw tea" simply refers to raw Pu-erh tea. Pu-erh tea is a type of Chinese tea that originates from Yunnan, China. However, in the present invention, the production area of the raw material of raw tea is not particularly limited, and tea from any production area can be used. Pu-erh tea is divided into ``ripe tea'' and ``raw tea.'' Both ``ripe tea'' and ``raw tea'' are manufactured through the same process until the middle, but the final process is different. Namacha is produced by maturing without fermentation by microorganisms.

The manufacturing process of pu-erh tea will be described below. Both ripped tea and raw tea are produced through bleached green tea, which is a type of green tea. Bleached green tea is produced by subjecting the plucked tea material, which is the raw material, to the steps of killing blue, rolling, and drying in this order. The tea material used as the raw material is not particularly limited as long as it is a generally cultivated tea variety, and one or more of them can be appropriately selected and used. The part of the tea material used as the raw material is mainly the leaves. However, portions other than leaves, such as tea leaf stalks, young branches, and stems, may be mixed.

(kill blue)
Killing is the process of applying heat to plucked tea leaves to inactivate the action of the oxidizing enzyme contained in the tea leaves themselves. To heat tea leaves while mixing the tea leaves put in a kettle, mixer or the like by hand or machine. In the pu-erh tea sterilization process, it is preferable not to completely inactivate the oxidase. Therefore, the temperature of the tea leaves during heating is preferably 60 to 80° C., which does not completely inactivate the oxidase.

(Kneading)
The tea leaves that have undergone the killing process are kneaded in the kneading process. The kneading process destroys the cells of the tea leaves and softens them, making it easier to extract the ingredients when the tea is extracted. The kneading step may be performed by manual kneading or mechanical kneading. It is preferable to adjust the intensity and degree of rubbing according to the type of tea leaves.

(dry)
The tea leaves that have undergone the rolling process are dried in the drying process. Drying methods include sun drying, natural drying, and mechanical drying. Drying also kills the blue, and the degree of killing the blue is moderate, so sun drying is most preferable. On days when the weather is bad, you can dry naturally indoors. The drying time can be 1 to 2 days, and the moisture content of the tea leaves after drying is preferably 15% or less, more preferably 10% or less. The tea leaves that have been dried are called bleached blue hair tea and are used as raw materials for pu-erh tea.

(rolling)
In the case of raw pu-erh tea, bleached blue hair tea is placed in a bag or mold, and while steaming, pressure is applied to form a disk or block to harden. This rolling process is an important process to separate raw tea from simply stale green tea. By rolling, the surface area of the tea leaves exposed to air is extremely reduced, and during the long-term aging, the components and flavor gradually change, transforming bleached green tea (green tea-like tea leaves) into raw tea. be able to.

(Aging)
The pressed pu-erh tea is left in a well-ventilated place to mature and become raw tea. During the maturation period, oxidative fermentation proceeds slightly due to oxidases remaining in the tea leaves, which were not inactivated by killing the tea leaves. The aging process takes a long time, and the raw tea used in the present invention is aged for at least 1 year or more, preferably 1.5 years or more, more preferably 2 years or more. It is believed that the long-term aging brings the components contained in the raw tea obtained after aging into a well-balanced state, and the interaction between the components enhances the effect of the carbohydrate absorption inhibitor of the present invention. Although there is no particular upper limit for the aging period, the aging period is preferably 8 years or less, more preferably 8 years or less, because the ingredients reach a limit where the ingredients do not change even if the tea leaves are left unattended, and the longer the aging period, the rarer and more expensive it becomes. 5 years or less. Namacha that has undergone the aging process is shipped as disc-shaped or block-shaped konatsucha (tea in a compacted state).

The above is the production process of raw tea. If the raw tea contained in the carbohydrate absorption inhibitor of the present invention contains an active ingredient that exerts a carbohydrate absorption inhibitory effect, the production process is as described above. For example, commercially available green tea may be used as a raw material for the carbohydrate absorption inhibitor of the present invention.

(Manufacturing process of ripe tea)
For comparison with raw tea, the manufacturing process of ripe tea will also be explained below.
Ripened pu-erh tea is also manufactured in the same process as raw tea up to the drying process, that is, the process of obtaining bleached blue-green tea. In the case of ripe tea, a process called tsutsui follows. In the tsutsui process, bleached green tea leaves soaked with water are artificially fermented at a suitable temperature by microorganisms such as koji mold and lactic acid bacteria, and finally ripe tea is obtained. Microbial fermentation decomposes the tea leaves, making it easier to extract with hot water. After the piled-up process, the tea leaves are dried, sorted, blended, etc., and then processed as sancha (distributed tea leaves). It is shipped as a block-shaped strained tea.

Nama-cha needs to be aged for at least one year or more to produce, whereas rip-cha can be produced by the tsutsui process for about 30 days. There is, and what is generally distributed as 'pu-erh tea' is ripe tea unless it is specified as 'raw tea'. As raw tea used in the carbohydrate absorption inhibitor of the present invention, commercially available raw tea may be used. Use what is available.

The carbohydrate absorption inhibitor of the present invention may contain raw tea. Namacha may be contained as it is, or pulverized namacha, an extract, or the like may be contained. Powders, granules and the like can be mentioned as pulverized products. The extract is obtained by immersion in an appropriate solvent at room temperature or in a heated state, solvent extraction using an extraction device such as a Soxhlet extractor, extraction by a distillation method such as steam distillation, extraction by compression method, etc. be able to. Solvents used for extraction include water, ethanol, hydrous ethanol, vegetable oils, and the like. The extract may be used as a diluent obtained by diluting the extract with an appropriate solvent, may be used as a concentrated concentrate, or may be prepared as a dry powder or paste. Dry powders may be dried by freeze-drying, spray-drying, or the like.

In the present invention, "suppression of carbohydrate absorption" means suppression of carbohydrate absorption in the digestive organs. In the present invention, "sugar" refers to carbohydrates excluding indigestible dietary fiber, such as monosaccharides such as glucose; disaccharides such as sucrose, lactose and maltose; oligosaccharides; and starch and glycogen. and other polysaccharides.

In the examples of the present application to be described later, by measuring the concentration of glucose in portal vein blood that sends nutrients from digestive organs such as the stomach and small intestine to the liver, the influence of changes in blood sugar levels due to liver metabolism is eliminated, and glucose in the digestive organs is measured. Suppression of quality absorption is determined. As shown in the examples, raw tea components have the effect of significantly suppressing the absorption of carbohydrates in the digestive organs. Therefore, the carbohydrate absorption inhibitor of the present invention can suppress the absorption of carbohydrates in the digestive organs, thereby preventing damage to blood vessels and exhaustion of the pancreas due to excessive blood sugar. In addition, it is possible to prevent, alleviate or treat various lifestyle-related diseases such as diabetes, hyperglycemia, obesity, hyperlipidemia, and arteriosclerosis by suppressing carbohydrate absorption.

The content of raw tea in the carbohydrate absorption inhibitor of the present invention may be appropriately contained within the range in which the effect is exerted. It is preferably 0.01 to 100% by mass, more preferably 0.1 to 90% by mass, even more preferably 1.0 to 80% by mass, relative to the total agent.

The carbohydrate absorption inhibitor of the present invention can itself be used as a carbohydrate absorption inhibitor, and can also be used to treat diseases caused by excessive carbohydrate absorption such as diabetes, hyperglycemia, obesity, hyperlipidemia, The carbohydrate absorption inhibitor of the present invention can be blended in order to produce an agent for preventing, alleviating or treating various lifestyle-related diseases such as arteriosclerosis.

The carbohydrate absorption inhibitor of the present invention can be used by blending it as an active ingredient in pharmaceuticals, foods, or feeds for humans or animals other than humans.

When the carbohydrate absorption inhibitor of the present invention is used as a pharmaceutical, the dosage form includes, for example, aerosols, liquids, capsules, granules, pills, powders, tablets, syrups, oral administration, injections, and suppositories. parenteral administration such as transdermal absorption agents, external preparations, etc., but oral administration is preferable because it has a high carbohydrate absorption inhibitory effect in the digestive organs. In addition, when the carbohydrate absorption inhibitor of the present invention is used as a food or feed such as a nutritional supplement, the same form as the above-mentioned pharmaceutical preparation for oral administration (aerosol, liquid, capsule, granule, pill, powder) , tablets, syrups, etc.).

Formulations of the various dosage forms described above may be prepared by adding other pharmaceutically acceptable excipients, binders, fillers, disintegrants, It can be prepared by appropriately combining surfactants, lubricants, dispersants, buffers, preservatives, flavoring agents, fragrances, coating agents, carriers, diluents and the like.

In addition, the carbohydrate absorption inhibitor of the present invention is labeled to the effect that it is used for the suppression of carbohydrate absorption, or is used for diseases caused by excessive carbohydrate absorption, such as diabetes, hyperglycemia, obesity, and hyperlipidemia. , Dietary supplements, functional foods, foods for the sick, and foods for specified health uses that are labeled as being used for reducing the risk of developing, preventing, alleviating, or treating various lifestyle-related diseases such as arteriosclerosis. The carbohydrate absorption inhibitor can be blended with foods such as

When the carbohydrate absorption inhibitor of the present invention is contained in a food as an active ingredient, the food includes breads, cakes, noodles, confectionery, frozen foods, ice creams, dairy products, beverages, and various other foods. In addition to food products, foods in the same forms as the above-mentioned orally administered pharmaceutical preparations (aerosols, liquids, capsules, granules, pills, powders, tablets, syrups, etc.) can be mentioned.

To prepare various forms of food, sugar absorption inhibitors can be used alone or in combination with other food ingredients, solvents, softeners, oils, emulsifiers, preservatives, fragrances, stabilizers, coloring agents, antioxidants. , humectants, thickeners and the like can be used in combination as appropriate.

The dosage or intake of the carbohydrate absorption inhibitor of the present invention may vary according to the patient's or consumer's condition, body weight, sex, age or other factors. Tea is preferably ingested in an amount of 30 mg to 5,000 mg, more preferably 200 mg to 2,000 mg, and more preferably 500 mg to 1,500 mg, based on dry mass. Amount is more preferred.

In addition, the carbohydrate absorption inhibitor of the present invention is preferably administered or taken before eating/feeding, during eating/feeding, or after eating/feeding. Administration or intake within minutes to 30 minutes after eating/feeding is preferred.

Subjects for administration include general healthy subjects, as well as patients with various lifestyle-related diseases such as diabetes, hyperglycemia, obesity, hyperlipidemia, and arteriosclerosis, and those at risk of developing these diseases. It can be expected to have a preventive effect on healthy people and reserves, and an improvement effect on patients.

(Sample preparation)
1. Preparation of Raw Tea Sample 10 g of raw Pu-erh tea leaves (originating from Yunnan, China, aged for 2 years) were boiled in 200 ml of hot water for 2 minutes for extraction. The extract was suction filtered and freeze-dried. Distilled water was added to the dried product to prepare a 10% by mass aqueous solution based on the weight of the dried product, which was used as a green tea sample in the following tests.

2. Preparation of ripe tea sample From 10 g of tea leaves of ripe pu-erh tea (origin to Makinohara City, Shizuoka Prefecture, Arahataen Co., Ltd., product name “Charyu Sullen”, black koji mold fermentation), 10 tea leaves were prepared in the same manner as the above raw tea sample. A mass % aqueous solution was prepared and used as a ripe tea sample in the following tests.

(experimental animal)
4-week-old rats were preliminarily bred for 4 weeks by giving solid feed and water ad libitum, and after being bred until 8-week-old, they were subjected to the following tests.

(Sugar absorption inhibition test)
By the method described in Japanese Patent No. 5435689, a catheter for collecting portal vein blood was placed in the portal vein of rats and a catheter for injecting feed was placed in the stomach of rats. According to the above method, dedicated catheters are inserted into the stomach and the portal vein, respectively, and a sample is administered from the stomach to collect the portal vein blood. Therefore, the components absorbed in the digestive organs can be directly measured. . According to the above method, rats were anesthetized with laughing gas/oxygen/fluthane mixed gas, and a sample injection catheter was placed in the stomach and a blood collection catheter was placed in the portal vein. Rats with indwelling catheters in the stomach and portal vein were randomly selected and divided into a "raw tea sample administration group" and a "ripe tea sample administration group" of 6 rats per group, and individually placed in cages for 24 hours. The mice were reared, and solid feed and water were given ad libitum. After these rats were fasted for 16 hours, a 15% by mass sucrose aqueous solution was continuously intragastrically administered through a sample injection catheter at a rate of 11.25 mL/kg/hr. Since the portal vein plasma glucose concentration was maintained at a constant level 60 minutes after the start of continuous administration of glucose, 120 minutes after the start of continuous administration of glucose, 7.2 mL/kg It was administered intragastricly through an infusion catheter. 0.05 mL of portal vein blood was collected from the blood collection catheter every 10 minutes until 60 minutes from 0 minute when the sample was administered. The collected blood was centrifuged to obtain plasma, and plasma glucose concentration was measured at each time point. FIG. 1(a) shows changes in portal vein plasma glucose concentration in the raw tea sample administration group, and FIG. 1(b) shows changes in portal vein plasma glucose concentration in the ripe tea sample administration group. As a result, in the raw tea sample administration group, the portal vein plasma glucose concentration at 10, 20 and 30 minutes after administration of the sample was compared with the value of glucose concentration in portal vein plasma before administration of the sample (0 minute). Glucose concentration values were significantly reduced. That is, the administration of the raw tea sample sustained the carbohydrate absorption inhibitory effect in the digestive organs for 30 minutes after administration. On the other hand, in the aged tea sample-administered group, no decrease in portal vein plasma glucose concentration was observed after sample administration. Statistical processing was performed by multiple comparison test (Bonferroni/Dunn method).

The carbohydrate absorption inhibitor of the present invention exerts an excellent effect of suppressing carbohydrate absorption in the gastrointestinal tract, and is useful in diseases caused by excessive carbohydrate absorption such as diabetes, hyperglycemia, obesity, hyperlipidemia, It can be used for reducing, preventing, mitigating or treating the risk of developing various lifestyle-related diseases such as arteriosclerosis.

Claims (3)

A carbohydrate absorption inhibitor containing pu-erh tea as an active ingredient,
The sugar absorption inhibitor, wherein the pu-erh tea is raw tea aged for two years . 2. The carbohydrate absorption inhibitor according to claim 1, which is for oral administration or ingestion. 3. The carbohydrate absorption inhibitor according to claim 1, which is in the form of an aerosol, liquid, capsule, granule, pill, powder, tablet or syrup.

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