JP6486724B2 - Pills for diet - Google Patents

Description

  The present invention relates to a tablet for dieting, wherein the surface of the tablet is coated with Gymnema acid or Gymnema sylvestre extract.

In recent years, the increase in the number of patients with lifestyle-related diseases has been regarded as a problem. Lifestyle-related diseases are names and concepts for referring to various diseases that occur due to lifestyle. Lifestyles include eating, water, smoking / non-smoking habits, exercise / no exercise habits, and so on. Particularly in Japan, it has been pointed out that dietary habits have become westernized (such as increased intake of meat), contributing to an increase in lifestyle-related diseases.
In Japan, cancer, cerebrovascular disorder, heart disease, etc. are mainly pointed out as diseases caused by lifestyle habits, and these are the three leading causes of death among Japanese people. Obesity increases the risk of developing these diseases. Obesity itself is also considered as a lifestyle-related disease, and for healthy living, countermeasures for obesity and prevention of obesity are recommended (a syndrome associated with obesity is also called metabolic syndrome).
Obesity has been common since middle age, with statistics showing that over 30% of men in their 40s and 70s are obese and 20-30% of women are obese. Obesity has been confirmed to increase the risk of these diseases, including the so-called three major causes of death of cancer, heart disease, and cerebrovascular disorders. Obesity is caused by excessive consumption of carbohydrates and increased consumption of greasy sweets and sweet drinks in the diet. “Eating habits guideline” and “meal balance guide” are formulated for the purpose of improving the situation of such eating habits, but it is difficult to change daily eating habits.
For this reason, dietary supplements are widely used as health supplements. Gymnema sylvestre extract is used as a useful ingredient in dietary supplements. It is known that Gymnema sylvestre extract inhibits sugar absorption by acting on the sweet taste receptor T1R2 / T1R3 in the digestive tract of Gymnema acid contained in the extract of Gymnema Sylvestre. For this reason, Gymnema sylvestre extract is often included in diet foods. In addition, it is known that this T1R2 / T1R3 receptor is present in the taste buds in the oral cavity, and when gymnemaic acid is bound to this receptor, only the sweetness of the taste is not specifically felt. And since sweetness cannot be felt, a meal is felt unsatisfactory, and as a result, the amount of meal intake decreases, and a diet effect is exhibited by suppressing absorption of carbohydrates and reducing the intake of foods containing sweetening ingredients. As a simple dietary supplement that exhibits such effects, Gymnema tea obtained by drying the leaves of Gymnema sylvestre is well known.

  Gymnema tea is recommended to be taken before meals, but is often not preferred due to its strong bitterness. However, when drinking Gymnema tea, sweetness is not felt for about 30 minutes thereafter, and the appetite decreases because the taste of the meal is lost.

Patent Document 1 discloses a method for producing a product that reduces the bitterness by reducing a gymnema acid or a gymnema sylvesta extract into a chewing gum or a troche, thereby reducing appetite thereafter.
Patent Document 2 describes a technique for removing bitterness by hydrolyzing Gymnema sylvestre leaf extract under alkaline conditions. In addition, a technique of inclusion water-solubilization with cyclodextrin is described in order to suppress precipitation of the substance from which this bitter taste has been removed.
Patent Document 3 describes a technique for producing a composition that eliminates both the bitterness and sweetness-inhibiting action of the Gymnema sylvestre extract by inclusion of the Gymnema sylvestre extract with cyclodextrin.

JP 07-184548 A Japanese Patent Laid-Open No. 06-321797 Japanese Unexamined Patent Publication No. 01-120263

The inventors of the present invention have been diligently researching foods that take advantage of this action, focusing on the strong sweetness-suppressing effect and diet effect of the above-described Gymnema acid or Gymnema sylvestre extract.
The main ingredients of food are protein, fat, and carbohydrate. The carbohydrate contains a sweetening ingredient as a carbohydrate, and its ingredient and amount are important elements of the deliciousness of the food. Also, beer, whiskey, sake, and soft drinks contain sugar, which is an important element of taste.
In general, in order to prevent obesity in eating, it is necessary to reduce the amount of food that is consumed, as well as the amount of fats and sugars that are components of those foods, as described above, as well as suppression of absorption of the consumed components. It is considered important.

  When ingesting food, the present inventor takes dietary supplements immediately before he / she does not feel a sense of avoidance such as special bitterness in order to ingest foods in a restraint manner. By reducing or avoiding the sweetness of foods eaten within a certain period of time immediately after that, the desire to eat sweet foods can be suppressed, and the avoidance feeling can be increased, We are researching a formulation that can provide reduced appetite.

  That is, the present invention limits the appetite well by reducing the food intake by an exogenous action of suppressing the sweetness sensation when ingesting food, and further absorbing the ingested food in the digestive tract. By suppressing this, an efficient diet is enabled. As a preparation for such a diet, when the tablet is ingested by coating the surface of the tablet consisting of ingredients that suppress absorption in the digestive tract of food with a gymnemaic acid or Gymnema sylvesta extract together with cyclodextrin, it is ingested thereafter It has been found that food intake needs can be reduced and absorption of food components can be suppressed.

  An object of the present invention is to form a water-soluble coating layer containing a gymnemaic acid or a gymnema sylvesta extract as a preparation that suppresses sweet taste without feeling bitter when ingesting a tablet, and an absorption suppressing ingredient for food ingredients in the inner core It is an object of the present invention to provide a novel tablet for diet having a two-layer structure.

The main configuration of the present invention is as follows.
(1) and gymnemic acid or Gymnema sylvestre extract the aqueous enteric coating layer of the tablet comprising a water-soluble coating layer and the inner core and the cyclodextrin is contained, the structure components in the inner core having a diet effect is contained a tablet agent that Yusuke contain 0.1~3mg per tablet to gymnemic acid or Gymnema sylvestre extract 0.1~3mg per tablet a water-soluble coating layer, the cyclodextrins water-soluble coating layer Furthermore, a tablet containing gymnema acid or Gymnema sylvestre extract and cyclodextrin in a ratio of cyclodextrin of 0.25 to 0.5 with respect to Gymnema acid or Gymnema sylvesta extract 1 .
(2) The tablet according to (1), wherein the water-soluble coating layer is a hydroxypropylmethylcellulose (HPMC) layer.
(3) The tablet according to (1) or (2), wherein the component having a diet effect is a component that exhibits an absorption inhibitory action on food components.
(4) The component according to any one of (1) to ( 3) , wherein the ingredient having a diet effect is one or more substances selected from Gymnema sylvestre extract, mulberry leaf extract, green tea extract, chitosan, kidney bean extract tablet.
(5) The tablet according to any one of (1) to ( 4) , wherein the inner core is shellac-coated.
(6) The tablet according to any one of (1) to ( 5) , which is a preparation for ingestion immediately before eating and drinking.

  According to the present invention, an ingredient for suppressing absorption of food ingredients and a water-soluble coating layer containing Gymnema acid or Gymnema sylvesta extract and cyclodextrin as an ingredient for suppressing subsequent sweet sensation without feeling much bitterness when taking tablets A novel tablet for diet consisting of is provided.

It is a schematic diagram which shows the structure of the tablet of an Example.

The present invention is a tablet comprising a water-soluble coating layer and an inner core, wherein the water-soluble coating layer contains Gymnema acid or Gymnema sylvesta extract and cyclodextrin, and the inner core contains a component having a diet effect. It is a tablet characterized by being.
When a diet component is blended with the tablet of the present invention, a diet component that continuously acts on the inner core is blended to suppress digestion and absorption in the stomach, duodenum, and small intestine of the ingested food. When Gymnema acid or Gymnema sylvesta extract and cyclodextrin, which are ingredients contained in the water-soluble coating layer, contain tablets in the mouth, the sweet taste receptor of miso is blocked by Gymnema acid, but coexists with cyclodextrin. It works so as not to feel bitterness. When the sweet taste receptor of the miso is blocked, the sweetness inherent in the food cannot be sensed, so that the taste of the food is changed, and the amount of food consumed decreases to reduce appetite.
In the tablet of the present invention, 0.1 to 3 mg of Gymnemaic acid or Gymnema sylvestre extract is blended per tablet in a water-soluble coating layer. In addition, it is not preferable that the content of Gymnema acid or Gymnema sylvestre extract contained in the water-soluble coating layer is less than 0.1 mg per tablet because the sweetness suppressing action is lost. Moreover, even if the content of Gymnema acid or Gymnema sylvestre extract exceeds 3 mg per tablet, the sweetness-inhibiting action is not changed, and a bitter taste is felt, which is not preferable.
The cyclodextrin is preferably blended in an amount of 0.25 to 1 times the cyclodextrin when the content of the Gymnema acid or Gymnema sylvesta extract is 0.1 to 3 mg of cyclodextrin per tablet. If it is 0.25 times or less, the bitter taste of Gymnema is strongly felt, and if it exceeds 1 time, sweetness may not be suppressed, so care should be taken.
In addition, the component mix | blended with the inner core of the tablet of this invention is one or more substances selected from Gymnema sylvestre extract, mulberry leaf extract, green tea extract, chitosan, and kidney bean extract. These components suppress digestion and absorption from the upper gastrointestinal tract to the end of the small intestine and exert a diet effect.

  For the water-soluble coating layer, water-soluble polymeric polysaccharides and cellulose derivatives can be used. Examples of the polymer polysaccharide include alginic acid, alginate, mannan and chitosan. Examples of cellulose derivatives include hydroxypropylcellulose (HPC) and hydroxypropylmethylcellulose (HPMC). As a component of the water-soluble coating layer used in the present invention, HPMC is particularly preferable. HPMC is a cellulose ether in which a 2-hydroxypropyl group is introduced into methylcellulose (MC), and sodium carboxymethylcellulose (CMC-Na) and carboxymethylcellulose calcium (CMC-Ca) listed in the Food Additives Official Document. Cellulose derivatives (cellulose ethers) in the same category, and widely used as capsule bases, tablet binders, or coating agents for general food additives or dietary supplements, mainly in Europe and the United States, as well as methylcellulose. ing. For general foods, for example, it is used as an edible film, frozen pizza (preventing moisture transfer from topping to dough, maintaining topping shape), nut products (antioxidant effect), meat products (preventing water retention and fading) ), French fries (prevention of oil absorption), etc.

The water-soluble coating layer is 0.5 to 10% by mass, preferably 1.0 to 5.0% by mass, based on the tablet weight. The water-soluble coating layer may contain a plasticizer such as glycerin, a high-sensitivity sweetener, or a masking agent such as lecithin, if necessary, in addition to the above-described Gymnema acid or Gymnema sylvesta extract and cyclodextrin. . What is necessary is just to set the compounding quantity of a masking agent according to the characteristic of the functional component to mix | blend.
The coating operation can be performed by a known gelation coating method performed for producing an enteric tablet. Moreover, the method used for the coating of a sugar-coated tablet may be sufficient.
According to Patent Document 3, it is described that inclusion of Gymnema sylvestre extract with cyclodextrin loses the bitterness and sweetness inhibiting action peculiar to Gymnema acid. However, when the cyclodextrin and Gymnema acid or Gymnema sylvestre extract are simply mixed as in the present invention, the bitter taste disappears as shown in the test examples, but the sweetness suppressing action does not disappear.

  It is preferable to apply a water-insoluble coating such as shellac or zein between the water-soluble coating layer and the inner core tablet to be coated, if necessary. Since the water-soluble coating layer has a low hygroscopic effect and masking effect, it is necessary to protect and mask with a water-insoluble coating layer when a highly hygroscopic component or a bitter / astringent component is added to the inner core. is there. Especially in the case of diet tablets, when substances with absorption-inhibiting action are blended, a non-water-soluble coating with shellac is applied so that these substances are not released in the oral cavity and cause discomfort. It is preferable to form a water-soluble coating layer.

Gymnema acid or Gymnema sylvestre extract contained in the water-soluble coating layer is extracted from the natural plant Gymnema sylvestre (Japanese name: Horaia Okazura). The triterpene compound obtained by purifying the extract is gymnemic acid. In the present invention, purified gymnemaic acid can be contained, but an unpurified Gymnema sylvestre extract may be contained.
This Gymnema sylvestre extract is obtained by extracting dry leaves of Gymnema sylvestre with, for example, an aqueous solution containing water or alcohol, and the above-mentioned unpurified Gymnema sylvestre extract is 1 kg of dry leaves of Gymnema sylvestre. 11 times amount of an aqueous solution containing 30% ethanol was added to the solution, extracted at 80 ° C. for 2 hours, the leaves were filtered off, the solution was concentrated, and powdered by spray drying to obtain a solid content of about 250 g. . Gymnemic acid is considered to be a compound having triterpene as a skeleton and glucuronic acid, but it is a glycoside containing 20 or more homologs, and a quantitative method has not yet been established. Specifically, it is defined as a Gymnema sylvestre extract precipitated at pH 3 or lower and extracted with a 30% -70% alcohol solution. In addition, when the preparation of the present invention is used for dieting, a substance having an effect of raising body temperature can be further blended in order to enhance the feeling of use if necessary. As the substance having a body temperature increasing action, any one or more of black ginger extract, ginger extract, and hihatsu extract can be blended.

  The cyclodextrin used in the present invention can be either powder or liquid. Further, known α, β, and γ types can be appropriately selected, and γ cyclodextrin is particularly preferable. Further, it may contain a linear dextrin.

  Black ginger (black ginger) is a plant belonging to the genus Banturmaceae, and its scientific name is Kaempferia parviflora, which is distributed in Southeast Asia such as Thailand and is easily available from this region It is. As for the extract of black ginger, an extract extracted using water, a hydrophilic organic solvent, or a mixed solvent thereof is commercially available from Maruzen Pharmaceutical Co., Ltd., and may be used.

  Ginger is a plant of the ginger family, and a pungent component, shogaol or (6) -shogaol, is produced when ginger is dried or heated. Gingerol is known to have an effect of improving blood flow, and a ginger extract containing gingerol is commercially available from Ikeda Sakuka K.K. and may be used.

  Hibatsu (Pipe longum) is an evergreen vine that is distributed in Southeast Asia belonging to the genus Pepperaceae. The fruit spikes are thick and cylindrical, and are used as spices. The most preferred site for the use of baboons in the present invention is fruit spikes, but roots, leaves, stems, flowers, or mixed sites thereof can also be used. As for the Hihatsu extract, an extract extracted using water, a hydrophilic organic solvent, or a mixed solvent thereof is commercially available from Maruzen Pharmaceutical Co., Ltd., and this may be used.

In the present invention, the diet effect can be further promoted by blending the inner core with a component that inhibits digestion and absorption of food components. Examples of these components include one or more substances selected from Gymnema sylvestre extract, mulberry leaf extract, green tea extract, chitosan, and kidney bean extract.
Mulberry leaf extract is an extract extracted from the leaves of mulberry (Moorus sp.) With water or alcohol. Mulberry leaf extract contains a component unique to mulberry called DNJ (1-deoxynojirimycin). This DNJ is an inhibitor of sucrase and maltase, which are small intestinal disaccharide-degrading enzymes, and has an effect of suppressing an increase in blood sugar level. It is known (Y. Yoshikuni: Agric. Biol. Chem. 52, (1), 121 (1988)). Currently, common mulberry leaf extracts are extracted from mulberry leaves with water, alcohol or a mixed solution thereof, and commercially available products such as “DNJ extract powder” and “DNJ extract B25” (both manufactured by Toyota Ma Health Foods Co., Ltd.) These are blended in products such as tea and tablets and used as food.

  Green tea extract is a hot water extraction fraction of tea (Camellia sinensis L.), and is an extract obtained by removing caffeine. In the tea extract, polyphenol compounds such as (+)-catechin, (+)-gallocatechin, (−)-gallocatechin gallate, (−)-epicatechin, (−)-epicatechin gallate, (−) − It contains high concentrations of epigallocatechin, (-)-epigallocatechin gallate, gallic acid, free theaflavin, theaflavin monogallate A, theaflavin monogallate B, theaflavin digallate, etc. Promotes metabolism. A green tea extract for diet purposes is sold, for example, by Taiyo Kagaku Co., Ltd. under the trade name of Sanphenon, and can be used.

  Chitosan is a basic polysaccharide partially deacetylated by alkaline hydrolysis of chitin, which forms the exoskeleton of crustaceans, and attracts attention as a diet food because it takes in fat and suppresses intestinal absorption of fat. Has been. Chitosan, obtained from crab shell or shrimp shell, is commercially available from Katakura Chikkarin Co., Ltd., Koyo Chemical Co., Ltd., Dainichi Seika Kogyo Co., Ltd., Nippon Kayaku Food Techno Co., Ltd., Nippon Suisan Co., Ltd. This can be used.

The kidney bean extract is an extract extracted from white bean (Phaseolus vulgaris), which inhibits the activity of α-amylase, a digestive enzyme, as a starch blocking agent that inhibits the decomposition of starch into dextrin and glucose. It is confirmed that it works. It is a substance that is expected to have an effect on diabetes and obesity because it also works to moderate the absorption of glucose from the digestive tract into the blood. White bean extract is commercially available from Indina Japan Co., Ltd. as a diet material, and can be used.
One or more substances selected from Gymnema sylvestre extract, mulberry leaf extract, green tea extract, chitosan, kidney bean extract should be selected as appropriate according to the age, sex, weight, obesity, etc. of the person to be dieted Blended.

As described above, the inner core is coated with a shellac layer in the case of tablets containing gymnema or the like in the inner core. By shellac coating, components contained in the inner core are released in the small intestine and exert a digestive absorption inhibition function.
Shellac is an exudate of the scale insect, which is a natural material that is insoluble in water but soluble in organic solvents such as ethanol. Shellac is suitable as an enteric coating material because it is insoluble under acidic conditions but becomes soluble at pH higher than 6.5. Shellac coat has the property of not dissolving in the upper part of the intestine.
For coating with shellac, shellac is dissolved in ethanol or a suitable organic solvent and sprayed on the surface of the tablet as the core, or surface coating is performed using a sugar-coated tablet coating apparatus. The coating amount of shellac is 0.2 to 2.0 mass%, preferably 0.3 to 1.0 mass%, based on the tablet weight.

The test examples and examples of diet tablets are shown below, and the present invention is described in detail.
<Test example>
Confirmation test of cyclodextrin content optimum for masking bitterness A 2% aqueous solution of gymnemic acid was prepared, and γ-cyclodextrin was added to this aqueous solution so as to have various concentrations. A small amount of this solution was contained in the mouth, and then a 5% sucrose aqueous solution was contained in the mouth to confirm how the sweetness of sucrose changed. The test results are shown in Table 1 below.

  When the content of γ cyclodextrin was the same as that of gymnemic acid, the sweetness-inhibiting effect of gymnemic acid was completely masked. It was also found that when the content of γ cyclodextrin was 1/4 or less than that of gymnemic acid, the bitter taste of gymnemic acid was strongly felt.

<Example>
1. Production of Inner Core Tablet Each raw material weighed based on the formulation of Table 2 below reflecting the results of the above test examples was mixed with a V-type mixer to obtain a tableting powder.
Tablets were produced using a rotary tableting machine (manufactured by Hata Kogyo Co., Ltd .: HT-AP38-SII). A tablet for an inner core having a tablet weight of 250 mg and a hardness of about 10 kgf was obtained at a tableting speed of 30 rpm and a pressure of 1.3 t.

2. Shellac coating The inner core obtained above was coated with 1 mg (0.4%) of shellac per tablet using Rack Glaze 10E (10% strength shellac solution). As a coating machine, a Doure coater made by Paulek was used.

3. Water-soluble layer coating (Gimnema, γ cyclodextrin, HPMC layer)
Based on the formulation of Table 3 below, each raw material was mixed to prepare a coating solution, and the aqueous layer was coated in the same manner as 1 to prepare tablets for dieting.

4). Tablet effect test (1) Confirmation of inhibitory effect on bitterness and sweetness Four sensory evaluators included 4 tablets of Examples in their mouths for 20 seconds to test whether bitterness was felt. Then they were swallowed with water. Thereafter, a 5% sucrose aqueous solution was included in the mouth to evaluate whether sweetness was felt. In addition, following the drinking of the tablets, meals were taken and appetite was recorded.
(2) Results All the evaluators did not feel the bitterness of the tablets. Moreover, all the evaluators did not feel the sweetness of the 5% sucrose solution. All assessors also recorded a decrease in appetite. The cause was the effect of the loss of sweetness.
From the above test, the tablet of the invention suppressed sweetness despite masking the bitter taste of Gymnema contained in the water-soluble coating layer on the surface. It was also found that appetite declined.
Furthermore, it was expected to exert a diet effect by a component contained in the inner core that suppresses absorption in the digestive tract.

Claims (6)

Gymnemic acid or Gymnema sylvestre extract the aqueous enteric coating layer of the tablet comprising a water-soluble coating layer and the inner core and the cyclodextrin and is contained, that having a structure component to the inner core having a diet effect is contained a tablet agent contains 0.1~3mg per tablet to gymnemic acid or Gymnema sylvestre extract 0.1~3mg per tablet a water-soluble coating layer, the cyclodextrins water-soluble coating layer, further Gymnema A tablet containing acid or Gymnema sylvestre extract and cyclodextrin in a ratio of cyclodextrins of 0.25 to 0.5 with respect to Gymnema acid or Gymnema sylvestre extract 1 .   The tablet according to claim 1, wherein the water-soluble coating layer is a hydroxypropylmethylcellulose (HPMC) layer.   The tablet according to claim 1 or 2, wherein the ingredient having a diet effect is an ingredient exhibiting an absorption inhibitory action on food ingredients. The tablet according to any one of claims 1 to 3 , wherein the ingredient having a diet effect is one or more substances selected from Gymnema sylvestre extract, mulberry leaf extract, green tea extract, chitosan, and kidney bean extract. The tablet according to any one of claims 1 to 4 , wherein the inner core is provided with shellac coating. The tablet according to any one of claims 1 to 5 , which is a preparation for ingestion immediately before eating and drinking.