KR102251360B1 - Food composition and pharmaceutical composition for improvement, prevention or treatment of diarrhea and antidiarrhotica with orobol - Google Patents

Abstract

The present invention relates to a food composition for improving diarrhea and a pharmaceutical composition for preventing or treating diarrhea containing Orobol, characterized in that it exhibits superior antidiarrheal activity compared to conventional antidiarrheal agents, and exhibits an excellent diarrhea stopping effect. Compared to drugs, access to materials is high, and side effects in the body are small, so stability can be secured.

Description

Food composition and pharmaceutical composition for improvement, prevention or treatment of diarrhea and antidiarrhotica with orobol}

The present invention relates to a food composition for improving diarrhea and a pharmaceutical composition for preventing or treating diarrhea containing Orobol, and more particularly, to Orobol, characterized in that it exhibits superior antidiarrheal activity compared to conventional antidiarrheal agents. It relates to a food composition for improving diarrhea and a pharmaceutical composition for preventing or treating.

Diarrhea is generally an abnormal increase in the number of bowel movements and the amount of water contained in the stool, and may accompany fever, convulsions, and vomiting. Depending on the duration of symptoms, it can be divided into acute and chronic, and it is called chronic diarrhea when it lasts for more than 1 month.

Acute diarrhea is mostly infectious diarrhea caused by pathogens, and due to diarrhea, electrolytes (such as sodium and potassium, dissolved in water and dissociated into ions, exist inside and outside the body's cells and play an important role in maintaining life) and moisture. Loss occurs. In addition, acute diarrhea can be caused by a variety of pathogens, functional disruption of intestinal function and drug-related side effects. On the other hand, chronic diarrhea is mostly non-infectious, and may have various causes, such as drugs, digestive disorders, and bowel disease.

Diarrhea can be particularly fatal for infants and toddlers, with infants and toddlers suffering from diarrhea being severely dehydrated and thus face a major problem. In addition, diarrhea is common to cancer patients, and it has been reported that it can interfere with cancer treatment. In addition, various chemotherapy, radiation therapy, surgery, graft versus host disease (GVHD), bone marrow transplantation, or various infections have also been reported to induce diarrhea. In addition, it has been reported that bacterial pathogens can also cause diarrhea syndrome with a range of severe tissue damage or damage deficiency. Enterotoxicity-producing E. coli, which causes acute and severe diarrhea, has been reported to produce toxins that act by modulating biological activity among epithelial cells, thereby exerting this effect.

Current treatments for diarrhea consist of antibiotic treatment of the causative microorganism or pharmacological involvement of the pathophysiological action. Antidiarrheal drugs reduce diarrhea symptoms (diffuse density of bowel movements, frequency of bowel movements and excessive bowel weight) by affecting the intestinal passage, mucosal transport or lumen content. Opioids, such as loperamide, are the most useful antidiarrheal agents, and they work in combination with intestinal passage inhibition, pre-absorption and antisecretory effects. Other useful pharmacological therapies include alpha-adrenergic agents such as clonidine and somatostatin analogs. In addition to slowing passage, these drugs can modify mucosal transport, and their clinical use has been limited due to their non-specificity of action. Adsorbents (Kaopectate), bismuth (Pepto-Bismol), and stool quality modifiers are often used as adverse drugs, but their efficacy other than Pepto-Bismol has not been demonstrated in most cases. Therefore, there is an urgent need for a safe and effective natural composition for improving, preventing or treating diarrhea.

On the other hand, orobol is isoflavone contained in soybeans, but it is contained in a small amount, so there has not been much research on its physiological activity. The IUPAC name is '3-(3,4-dihydroxyphenyl)-5,7-dihydroxychromen-4-one', and its molecular weight is 286.23 g/mol. Genistein, a major soy isoflavone, exists as a monophenol-type structural material, and in the case of orobol, one more hydroxyl group is introduced at the ortho-position of such a monophenol-type structural material. Therefore, genistein, a representative isoflavone, can be bioconverted to obtain orobol.

In addition, orobol is known to be present in a small amount in Tempe, an Indonesian fermented soybean food, and is known to have an effect of inhibiting angiogenesis (Kiriakidis S. et al., Br J Nutr, 93(3):317). -23, 2005). However, until now, there is no known about a food composition for improving diarrhea and a pharmaceutical composition for preventing or treating diarrhea containing orobol.

In Korean Patent Registration No. 10-1602629 (registration date 2016.03.07), a method for preparing a composition for improving skin wrinkles containing Orobol is described. Korean Patent Registration No. 10-1587246 (registration date 2016.01.14) discloses a food composition for preventing metabolic diseases or a pharmaceutical composition for treating metabolic diseases containing orobol.

'Governor' refers to a drug that works on the intestine to stop diarrhea in the intestine. In a more comprehensive sense, it includes intestinal disinfectants, antibiotics, and sulfa drugs that act on bacteria that cause diarrhea.

Antidiarrheal agents can be used to alleviate diarrhea symptoms, and antidiarrheal agents include bowel movement inhibitors, fungicides, astringents, adsorbents, and intestinal agents, depending on the action of the drug. Among them, loperamide is a local government agency that the World Health Organization (WHO) notified of concerns about side effects of the central nervous system when fed to infants under 6 months of age. In addition, when administering this drug to children aged 2 to 5, the Ministry of Health and Welfare made sure to use it according to the instructions of a doctor or pharmacist, and to indicate a warning about possible sensitive reactions of the central nervous system such as muscle tone. Acrinol is an aromatic organic compound that is a derivative of acridine. This substance is a component of an abortion medicine and may cause miscarriage when taken by pregnant women. When smelting bismuth, it contains lead and cadmium, which can cause heavy metal poisoning.

Meanwhile, as a popular treatment for diarrhea in the related art, chemotherapeutic agents, astringent agents, atropine agents, and the like have been used depending on the cause. In addition, opiates and morphine are known to cause spasm of intestinal smooth muscle and ataxia of peristalsis, thereby exhibiting adipose action. However, since morphine is concerned about the risk of addiction, such as dependence due to the central action, the necessity of separating the central action and the intestinal action has been considered when using morphine as an antidiarrheal agent.

Accordingly, in order to solve such a problem, the present invention intends to develop and provide a food composition for improving diarrhea and a pharmaceutical composition for preventing or treating diarrhea containing Orobol, a natural material present in soybeans.

The present invention provides a food composition for improving diarrhea, characterized in that it contains orobol to provide.

The present invention provides an anti-diarrheal agent, characterized in that it contains orobol.

In the food composition and the branch preparation of the present invention, the Orobol may be derived from beans, for example.

In the food composition of the present invention, the food composition may preferably have a blood stool alleviation ability.

In the anti-diarrheal agent of the present invention, the anti-diarrheal agent may preferably have an ability to relieve blood stool.

The present invention provides an excellent diarrhea-stopping effect by providing a food composition for improving diarrhea and a pharmaceutical composition for preventing or treating diarrhea containing orobol, and has high accessibility to materials compared to synthetic drugs and has fewer side effects in the body to secure stability. There is a possible advantage.

1 is a graph showing the results of confirming the average weight loss alleviation effect of Orobol for each group.
2 is a graph showing the results of confirming the diarrhea and bloody stool alleviation efficacy of Orobol on average for each group.

The present invention provides a food composition for improving diarrhea, characterized in that it contains orobol to provide. In addition, the present invention provides an anti-diarrheal agent, characterized in that it contains orobol. The term "diarrhea" of the present invention refers to a drug that acts on the intestine to stop diarrhea in the intestine. Since the food composition and the anti-diarrheal agent of the present invention are based on natural products, there is an advantage in that the side effects in the body, which are the problems of the conventional anti-diarrheal agents, can be solved.

Orobol used in the present invention is a kind of isoflavone, and according to the following experiment in which Orobol was administered to a mouse that induces diarrhea, the effect of reducing weight loss and anti-diarrhea of Orobol was confirmed. Became. In particular, according to Example 1 below, the group to which Orobol was administered exhibited superior anti-diarrheal activity and blood stool relief effect than the control group. Accordingly, the present invention can provide a food composition and antidiarrheal agent for improving diarrhea of excellent efficacy, characterized in that it contains orobol.

In the food composition and the branch preparation of the present invention, the Orobol may be derived from beans, for example.

In the food composition of the present invention, the food composition may preferably have a blood stool alleviation ability.

In the anti-diarrheal agent of the present invention, the anti-diarrheal agent may preferably have an ability to relieve blood stool.

The formulation of the anti-diarrheal agent of the present invention is not particularly limited, but by adding various excipients commonly used in the anti-diarrheal agent, it can be formulated in any one of a coated tablet, a powder, a granule, and a capsule.

In the case of preparing coated tablets, talc, hydroxypropyl methylcellulose, and polyethylene glycol are added to Orobol, which is the main component, and then mixed and tableted by a known method, or lactose, magnesium snearate, and colloidal silicon dioxide are added to Orobol, which is the main component. , Hydroxypropyl methylcellulose, polyethylene glycol, and titanium oxide can be mixed and tableted by a known method.

In the case of preparing a powder, it can be prepared by a known method by adding sucrose, lactose, and microcrystalline cellulose to the main component, orobol, or by adding mannitol, corn starch, and colloidal silicon dioxide to the main component. I can.

In the case of preparing a granule, it can be prepared by a known method by adding sucrose and corn starch to the main ingredient, Orobol, or by adding mannitol, lactose, povidone, and colloidal silicon dioxide to the main ingredient. have.

When prepared as a capsule, microcrystalline cellulose, corn starch, hydroxypropyl cellulose, and magnesium stearate are added to the main component, orobol, by a known method, or lactose, povidone, colloidal silicon dioxide, talc, It can be prepared by a known method by adding magnesium stearate.

On the other hand, considering a single dose of a conventional anti-diarrheal agent, it is not desirable to extremely increase the content of the present invention Orobol, and the amount of the active ingredient added to a conventional anti-diarrheal agent (preferably 1-10 mg/kg BW, BW is an abbreviation of Body Weight, meaning'weight'), and it is desirable to take it once a day until the condition improves. However, such dosage may be adjusted by a specialist in consideration of the patient's weight, severity, and the patient's condition.

On the other hand, the food composition of the present invention is, for example, meat, grains, caffeine beverages, general beverages, chocolate, bread, snacks, confectionery, pizza, jelly, noodles, gums, ice cream, alcoholic beverages, alcohol, vitamin complexes and other health It may be any one selected from supplements, but is not necessarily limited thereto.

Hereinafter, the content of the present invention will be described in more detail through the following examples and experimental examples. However, the scope of the present invention is not limited to the following examples and experimental examples, and includes modifications of equivalent technical ideas.

[Experimental Example: in vivo The efficacy of orobol in improving bowel disease symptoms (weight loss, diarrhea, bloody stool)]

In this experimental example, an experiment was conducted to confirm the efficacy of orobol in improving bowel disease symptoms (weight loss, diarrhea, bloody stool).

1) Sample preparation and diarrhea

In order to test whether symptoms such as diarrhea and bloody stool are relieved through Orobol treatment, a total of 5 groups (Control, DSS, DSS+Genistin, DSS+Genistein, DSS) of 7-week-old male experimental mice (C57BL6), each 8 mice per group. +Orobol).

For each experimental group, excluding the control group (Control) and the induction group (DSS), 5 mg/in each of Genistin, Genistein, and Orobol were dissolved in a solution (PEG 300 97% + DMSO 3%). A ml stock was prepared, and this stock was administered once a day at a dose of 10 ml/kg BW per mouse (about 200 μl since the average mouse body weight is 20 g), and 50 mg/kg per day Genistin, Genistein, and Orobol of BW (here, BW is an abbreviation of Body Weight) were ingested, respectively, and were administered orally for a total of 13 days. . In other words, it was administered orally for a total of 13 days at a once/day dose of 50 mg/kg B.W. At this time, only the vehicle (PEG 300 97% + DMSO 3%) solution was administered to the control group (Control) and the induction group (DSS), and the same amount as added in the experimental groups was administered during the same period. All administration was performed using a syringe for oral administration.

The control, induction group, and experimental group samples were each pretreated for a week, and then Dextran sodium sulfate (DSS) was mixed in drinking water at a concentration of 2.5% as an inducing agent to induce acute diarrhea from the 8th day after starting the sample administration and supplied daily for 6 days. . Through this, an experimental mouse inducing diarrhea was produced.

2) Confirmation of the efficacy of orobol to relieve weight loss

When DSS causes diarrhea, weight loss occurs. Targeting the mouse (C57BL6) inducing diarrhea by the above method The weight of the experimental mice (C57BL6) was measured for 6 days every day starting from the day of administration of the inducer DSS, and the averages for each group were shown in FIG. 1.

As a result, as shown in FIG. 1, it was confirmed that the orobol group significantly reduced weight loss compared to the groups administered with DSS alone or DSS and other isoflavones (Genistin, Genistein, Orobol). (Significance compared of control: ## <0.01; compared of DSS: * <0.05) (Fig. 1)

[Example 1: Confirmation of diarrhea and blood stool relief efficacy of orobol]

In this example, an experiment was conducted to confirm the diarrhea and bloody stool relief effect of orobol.

Experimental mice administered with DSS show symptoms of diarrhea and bloody stool. On the last day of DSS administration for mice (C57BL6) inducing diarrhea in the same manner as in the above Experimental Example, separate experimental mice (C57BL6) one by one and look at the excreted feces, and the degree of diarrhea and bloody stool was scored according to the determined scoring. The degree of symptoms of diarrhea and bloody stool was measured. Diarrhea and bloody stool scoring criteria were measured by dividing into four steps as follows, and averaged for each group and described in FIG. 2 (diarrhea score: 0: normal stool; 1: soft stool; 2: very soft stool; 3: watery stool / Blood stool score: 0: normal colored stool; 1: brown stool; 2: mildly bloody stool; 3: bloody stool).

As a result of the experiment, as shown in FIG. 2, it was confirmed that the degree of diarrhea and bloody stool were alleviated in the orobol group compared to the groups administered with DSS alone or DSS and other isoflavones (Genistin, Genistein, Orobol). (Significance compared of control: ## <0.01; a-c: p <0.05)

Claims (6)

A food composition for alleviating weight loss and alleviating blood stool, characterized in that it contains orobol.
The method of claim 1,
The above aurobol,
Food composition for relieving weight loss and relieving blood stool, characterized in that derived from soybeans.
delete An antidiarrheal agent containing orobol, characterized in that it has the ability to alleviate weight loss and relieve blood stool.
The method of claim 4,
The above aurobol,
A branch made from soybeans.
delete

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