JP2007246488A - Peptic ulcer ameliorating composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a composition, especially food and beverage that are safe to human, animals, etc., is continuously ingested and has excellent prevention and/or amelioration action on peptic ulcer. <P>SOLUTION: The composition for preventing and/or ameliorating peptic ulcer comprises a sesamin. The composition contains 0.001-10 wt.% of a sesamin. An excellent peptic amelioration composition, especially food and beverage are obtained. The composition containing a sesamin is safely administered to human and animals. Consequently, the composition is continuously administered and is a composition for preventing and ameliorating peptic ulcer without causing a rebound. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

TECHNICAL FIELD OF THE INVENTION

  The present invention relates to a composition for improving peptic ulcer effective for the prevention and treatment of peptic ulcer, and more particularly to a composition containing sesamin as an active ingredient, and a food and drink containing the composition.

Conventional technology

  Peptic ulcer refers to ulcerative lesions of the upper gastrointestinal tract caused by autodigestion caused by acid or pepsin in the gastric juice, and actually means a chronic gastric / duodenal ulcer. It is a disease characterized by repeated relapses and chronic progress (Non-patent Document 1). It is widely accepted that peptic ulcers are caused by the fact that the balance between attack factors and defense factors is tilted toward the attack factors. Attack factors include hydrochloric acid, pepsin in gastric juice, increased gastric secretion by vagus nerve and gastrin, histamine, stress, drugs such as NSAIDs, etc. Defense factors include mucus, mucosal blood flow, secretin, somatostatin, etc. The control mechanism is raised. Furthermore, since the discovery of H.pyrori, H. pylori has also attracted attention as a major cause of peptic ulcer.

  According to the National Health Survey, the prevalence of peptic ulcer in Japan is 4.3% in 1980, 4.6% in 1985 (Non-Patent Document 2), and recently it is said to be about 2-3%. Although significant progress has been made in the treatment method, the number of operations has been greatly reduced, and most of them have been able to be cured. Has been. It is also true that ulcers due to stress and ulcers in the elderly are increasing due to westernization of eating habits, increased social anxiety, and extension of life expectancy.

  As therapeutic agents, H2 blockers, proton pump inhibitors, antacids, anti-pepsin agents, anticholinergic agents, antigastrin agents and the like are used clinically as aggressive factor inhibitors. On the other hand, mucosal protective agents, mucosal repair promoters, mucus production promoters, mucosal microcirculation improvers, prostaglandin synthesis promoters, prostaglandin preparations and the like are used as protective factor enhancers. Among them, H2 blockers such as cimetidine, which is an attack factor inhibitor, and proton pump inhibitors such as omeprazole are most widely used, and although they have remarkable therapeutic effects, they have major problems such as side effects and recurrence problems caused by long-term administration. Is left behind. Gastric acid plays an important role in the body, not only digesting food, but also protecting against external enemies such as bacteria and pathogenic microorganisms. After healing, these drugs that have a strong gastric acid secretion inhibitory effect must be discontinued. However, it is clear that rebounding gastric acid secretion and recurrence and worsening of ulcers are frequently observed after drug withdrawal. In addition, its use is restricted due to the problem of drug interaction with drugs other than peptic ulcer, and the appearance of side effects such as blood disorders is known. There has been a strong demand for the development of a safer and more effective preventive / ameliorating agent for gastrointestinal diseases. If you can find a substance that has a safe and effective action in natural food ingredients and has a preventive or ameliorating effect on peptic ulcer without side effects, you will be able to continue taking it even after healing. It is possible to maintain a healthy digestive tract without worrying about rebound or recurrence of gastric acid secretion.

Sesamin is a lignan compound peculiar to sesame contained in a small amount in sesame. The lignan compound is a generic name for compounds produced by oxidative condensation of a phenylpropane skeleton (C ₆ -C ₃ compound) as a unit. Some lignans are known to have an effect on peptic ulcers, such as neolignan derivatives (Patent Document 1), novel lignan derivatives in Schizandra chinensis Balii (Patent Document 2), and Euphorbiaceae A novel lignan compound (Patent Documents 3 to 4) in Mallotus anomalus Meer et chun has been developed as a pharmaceutical, and a lignan compound (Non-patent Document 3) in European yew (Taxus Baccata L.) and the like. . However, it is known that any of these compounds is completely different from sesamin, which is a lignan in sesame. In addition, Shishimi-Fuga, Tabuchi carrot, Chabotokeiso, Heraobako, Oawadachisou (patent document 5), catechin (non-patent document 4), grape seed protocyanidin (non-patent document 5), rose The Mary extract (patent document 6), Ezoukogi extract (patent document 7), etc. disclose the gastric acid secretion hormone inhibitory effect, gastric ulcer inhibitory action, and the like.

  The following physiological activities have been reported for sesamins. For example, from experiments using purified sesamin, metabolism inhibition of cholesterol or bile acids in the intestine (Patent Document 8), alcohol poisoning and alleviation of withdrawal symptoms (Patent Document 9), liver function improving action (Patent Document 8) Document 10), in vivo stabilization action of polyunsaturated fatty acids (Patent Document 11), Δ5-unsaturation enzyme inhibitory action (Non-Patent Documents 6 to 7, Patent Document 12), migraine suppression action (Patent Document 13) ), Apoptosis-inducing action on human leukemia cells (Patent Document 14), melatonin oxidative degradation inhibitory action (Patent Document 15), etc.

In addition, from experiments using sesame oil containing sesamin, it was found that inflammatory diseases (amyotrophic lateral sclerosis) were improved (Patent Document 16), anti-inflammatory and infection protective action (Patent Document 17), α-linolene. The allergy prevention or improvement action (patent document 18) etc. by combined use with the fats and oils which contain at least 1 sort (s) among an acid, eicosapentaenoic acid, and docosahexaenoic acid are clarified. However, the effects on gastric acid secretion or peptic ulcers have never been studied and are not known so far.
JP-A-62-209070 JP 63-30442 A Japanese Patent Laid-Open No. 3-81272 Japanese Patent Laid-Open No. 3-120264 JP 2005-320274 A JP 2000-72685 A JP 2002-3391 A Japanese Patent No. 3183664 U.S. Pat. No. 4,427,694 Japanese Patent No. 3075358 JP-A-11-269456 Japanese Patent No. 3070611 JP 2003-183172 A JP 2001-151676 A JP 2000-143546 A JP 2005-530442 A Japanese National Patent Publication No. 10-500937 JP-A-5-58902 Medical Dictionary, 18th edition, Nanzan-do (1998) Health and Welfare Statistics Association, National Hygiene Trends, 33 (9), 81-82 (1986) Gurbuz, I., et al., Z. Naturforsch., 59, 233-236 (2004) Sato, H., et al., J. Gastroenterol., 37, 106-111 (2002) Iwasaki, Y., et al., J. Gastroenterol., 39, 831-837 (2004) S. Shimizu, et al, J. Am. Oil Chem. Soc., 66, 237-241 (1989) S. Shimizu, et al., Lipid, 26, 512 (1991)

  Several substances have been proposed to improve peptic ulcers, especially extracts from natural products, but their effects are not always sufficient, and the safety of continuous intake has not been fully confirmed .

  An object of the present invention is to provide a composition, particularly a food and drink, which is safe for humans and animals, and thus can be continuously ingested and has an excellent effect of preventing and / or improving peptic ulcer. And

As a result of intensive studies to solve the above problems, the present inventors surprisingly,
It has been found that ingesting sesamin enhances the effect of suppressing peptic ulcer. Specifically, it has been found that by ingesting a composition containing an effective amount of sesamin, particularly a food or drink, the effect of preventing and / or improving peptic ulcer is achieved.

  In order to achieve this goal, we focused on gastrin and histamine as gastrointestinal hormones that control the secretion of gastric acid, an attack factor, and examined the effects of sesamin on these hormones. Gastrin is a gastrointestinal hormone released from the G-cells of the mucosal epithelium in the gastropyloric vestibule, which acts on gastric body wall cells to stimulate gastric acid secretion. Histamine is released from mural cells in the gastric mucosa and has an action of promoting gastric acid secretion. Therefore, the effects of sesamin on gastric acid secretion were evaluated using the isolated gastric reflux model of rats using the secretion amount of these gastrointestinal hormones as an index. As a result, sesamin suppressed the secretion of these hormones and eventually gastric acid. It was confirmed that the secretion was suppressed.

    Sesamin is a safe substance that has been ingested as a food and drink for many years, and various physiological activities are known. Therefore, since the composition containing sesamin can be expected not only to improve the peptic ulcer but also to exhibit the physiological activity of sesamin, it was confirmed that the composition was useful as a health food. It came to complete.

The present invention relates to a composition containing food and drink as follows.
1. A composition for improving peptic ulcer containing sesamin as an active ingredient.
2. 2. The composition for improving peptic ulcer according to 1 above, wherein the amount of sesamin compounded is 0.001 to 10% by weight, preferably 0.001 to 1% by weight.
3. 3. The composition for improving peptic ulcer according to 1 or 2 above, wherein the sesamin is a sesamin concentrate containing 1% by weight or more of sesamin.
4). 4. The composition for improving peptic ulcer according to 3 above, wherein the sesamin concentrate contains 20% by weight or more of sesamin.
5). The composition for improving peptic ulcer according to any one of the above 1 to 4, wherein the sesamin is sesamin and / or episesamin.
6). The composition for improving peptic ulcer according to any one of the above 1 to 5, which is in the form of food or drink.

BEST MODE FOR CARRYING OUT THE INVENTION

(Sesamin)
The sesamin used in the present invention includes sesamin and its analogs. Examples of the sesamin analog include episesamin and dioxabicyclo [3.3.0] octane derivatives described in JP-A-4-9331. Specific examples of sesamin can include sesamin, sesaminol, episesaminol, sesamorin and the like. Among these, sesamin and episesamin can be exemplified as a more preferred embodiment because of their strong physiological action among sesamins and high absorbability to living bodies.

  In addition, as long as the metabolite of sesamin shows the effect of this invention, it is a sesamin analog contained in the sesamin of this invention, and can be used for this invention.

  The sesamin used for this invention is not restrict | limited at all by the form, manufacturing method, etc. For example, when sesamin is selected as the sesamin, usually sesamin extracted from sesame oil by a known method (for example, the method described in JP-A-4-9331) (referred to as sesamin extract or purified product) Although it can also be used, commercially available sesame oil (liquid form) can also be used as it is. However, when sesame oil is used, the flavor unique to sesame oil may be evaluated as sensory unfavorable, so a tasteless and odorless sesamin extract (or purified sesamin product) extracted from sesame oil is used. It is preferable. Further, when sesame oil is used, since the sesamin content is low, an attempt to formulate a preferable amount of sesamin may cause inconvenience ingestion because the volume per unit dose of the composition becomes too large. In particular, when formulated for oral administration, preparations (tablets, capsules, etc.) per unit dosage become too large, resulting in trouble ingestion. Therefore, it is preferable to use a sesamin extract (or a sesamin purified product) from sesame oil from the viewpoint that the intake may be small.

  The daily dose of sesamin for sufficiently achieving the peptic ulcer improving action of the present invention is usually 1 to 60 mg, preferably 5 to 60 mg.

  The composition containing the sesamin of the present invention can be formulated into any dosage form. For example, it may be administered orally in the form of liquids, tablets, granules, powders, capsules, dry syrups, pills, etc., or in the form of injections, etc. It can be appropriately selected depending on the progress status and other conditions.

  Furthermore, the composition of the present invention is effective for preventing peptic ulcer and / or improving symptoms of peptic ulcer, especially chronic peptic ulcer, by daily use as a health food. . Moreover, since it is thought that various physiological actions other than the peptic ulcer improving action which sesamin has can be considered, this form as a health food is suitable. The health food here is, for example, a formulation or food containing the composition itself containing the sesamin of the present invention as an active ingredient, such as capsules and tablets, and the above-mentioned composition of the present invention as a general food. Functional foods (specific health foods and conditionally specified health products) that are added as ingredients to prevent and / or improve (treat) peptic ulcers on living bodies and various functions of sesamins. For example). Furthermore, foods characterized by being used to prevent or ameliorate peptic ulcer are also included.

  The form of the health food containing sesamin is not particularly limited. For example, it is a solid such as powder, granule or tablet; a liquid such as solution, emulsion or dispersion; or paste It can be prepared in any form such as a semi-solid form.

  In addition, other components having various functions such as vitamins, enzymes, dietary fiber, antioxidants, preservatives, stabilizers, dispersants, and other conventional components can be blended.

The invention is illustrated in more detail by the following examples.
[Example 1]
To achieve this goal, we focused on gastrin and histamine as gastrointestinal hormones that control the secretion of gastric acid, an attacking factor. Gastrin is a gastrointestinal hormone released from the G-cells of the mucosal epithelium in the gastropyloric vestibule, which acts on gastric body wall cells to stimulate gastric acid secretion. Histamine is released from mural cells in the gastric mucosa and has an action of promoting gastric acid secretion. Therefore, using the gastric hormone secretion as an index, we isolated gastric acid secretion of sesamin using a rat isolated gastric reflux model (Matsuno, M et al., J Gastroenterol., 32, 579-589, (1997)). The effect on the environment was evaluated.

  Five-week-old Wistar rats acclimated to the test environment for a certain period were randomly divided into two groups, one group being fed with a control diet and the other group being fed with a diet containing 0.2% sesamin for two weeks. Subsequently, isolated gastric reflux animals were prepared according to the previous reports. Specifically, the stomach / duodenum and blood vessels associated therewith were removed under Nembutal anesthesia, and then a polyethylene tube was inserted into the celiac artery and portal vein and fixed. Other arteries, veins and pancreas (tubes) were ligated and removed. The excised stomach was kept in Krebs Ringer-biocarbonate buffer (37 ° C., pH 7.4), and the gastric lumen was flushed with 1% HEPES at a constant rate. A reflux solution was flowed from the celiac artery side and collected on the portal vein side, and concentrations of various digestive hormones in the collected solution were measured by a radioimmunoassay (RIA) method.

As a result, it was revealed that the secretion of gastrin (FIG. 1) and histamine (FIG. 2) was suppressed in the sesamin intake group compared to the control group. From this, it is considered that sesamin has an action of suppressing the secretion of gastric acid and exhibits an inhibitory effect on peptic ulcer.
Example 2 Formulation Example (Formulation Example 1) Granule Sesamin 0.01 g
0.25 g of tocopherol acetate
Silica anhydride 20.5g
Corn starch 179.0g
After uniformly mixing the above powder, 100 ml of 10% hydroxypropylcellulose / ethanol solution was added, kneaded as usual, extruded and dried to obtain granules.

(Formulation Example 2) Capsule Gelatin 60.0%
Glycerin 30.0%
Methyl paraoxybenzoate 0.15%
Propyl paraoxybenzoate 0.51%
An appropriate amount of water The following composition was filled in a soft capsule skin made of the above-mentioned components by a conventional method to obtain 200 mg soft capsules.

Sesamin 10.0mg
Glycerin fatty acid ester 15.0mg
Beeswax 15.0mg
Wheat germ oil 250mg

(Formulation example 3) Tablet sesamin 0.01 g
282 g starch
Sucrose fatty acid ester 9.0g
9.0g of silicon oxide
These were mixed and tableted with a single-punch tableting machine to produce tablets with a diameter of 9 mm and a weight of 300 mg.

(Formulation example 4) Taste of drink agent: DL-sodium tartrate 0.1 g
0.009 g of succinic acid
Sweetness: 800g liquid sugar
Acidity: Citric acid 12g
Vitamins: Vitamin C 10g
Sesamin 1g
Vitamin E 30g
Cyclodextrin 5g
Fragrance 15ml
1g potassium chloride
Magnesium sulfate 0.5g
The above ingredients were blended and water was added to make 10 liters. About 100ml of this drink is drunk.

It is a figure which shows the gastrin density | concentration in an isolated gastric reflux liquid. It is a figure which shows the histamine density | concentration in an isolated gastric reflux liquid.

Claims (6)

A composition for improving peptic ulcer containing sesamin as an active ingredient. The composition for improving peptic ulcer according to claim 1, wherein the blending amount of sesamin is 0.001 to 10% by weight. The composition for improving peptic ulcer according to claim 1 or 2, wherein the sesamin is a sesamin concentrate containing 1% by weight or more of the sesamin. The composition for improving peptic ulcer according to claim 3, wherein the sesamin concentrate contains 20% by weight or more of sesamin. The composition for improving peptic ulcer according to any one of claims 1 to 4, wherein the sesamin is sesamin and / or episesamin. The composition for improving peptic ulcer according to any one of claims 1 to 5, wherein the composition is in the form of food or drink.

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