JPH0755909B2 - Amylase inhibitor - Google Patents

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a novel amylase inhibitor, and more particularly to an amylase inhibitor mainly composed of bay leaves or deoiled ones, and a food containing the same.

[0002]

2. Description of the Related Art In recent years,
In developed countries, various adult diseases are increasing due to causes such as overnutrition. Many of these adult diseases are caused by an increase in blood sugar due to excessive intake of starch and the like, and examples thereof include diabetes, obesity and arteriosclerosis.

In general, the treatment of such diseases mainly consists of dietary therapy, but in addition to causing mental distress to the patient, the burden of calorie calculation and the like is large. Therefore, as a simple method, when a starch food such as rice and udon, which is the center of Japanese dietary habits, is eaten, an amylase inhibitor is taken to inhibit the digestion of starch. That is, by inhibiting the action of amylase that digests starch, it is possible to suppress the digestive absorption of sugars and suppress the rise of blood sugar, and based on the idea that these metabolic diseases can be prevented and treated, several species have been recently developed. Amylase inhibitors have been discovered.

These amylase inhibitors are oligosaccharides and peptides obtained from microorganisms or cereals, but they have problems in terms of stability, safety and effectiveness of substances, and most of them are However, it has not yet reached the stage of practical use.

[0005]

[Means for Solving the Problems] Therefore, the inventors of the present invention have diligently studied in order to find a novel amylase inhibitor having no problem in terms of safety and efficacy for crude drugs that have been used for many years. As a result, they discovered that bay leaves had an amylase inhibitory action, and completed the present invention.

That is, the present invention comprises, firstly, an amylase inhibitor containing bay leaves as a main component. The present invention secondly comprises an amylase inhibitor whose main component is deoiled bay leaves. Thirdly, the present invention comprises a food product containing the bay leaves or deoiled products thereof.

The laurel leaf used in the present invention is a leaf of Laurus nobilis L. <Lauraceae>, an evergreen tall tree cultivated all over the world including the Mediterranean coast. The leaves may be raw or dry. Further, the leaves may be used in the form as they are, but may also be used by appropriately cutting them into fine powder and crushing or crushing them into powder.

The bay leaves used in the present invention are also deoiled. As a deoiling method, any known method can be used. For example, hexane,
There are a method of degreasing with an oil-soluble organic solvent such as acetone and ether, and a method of degreasing by steam treatment such as steam distillation and autoclave treatment. The amylase inhibitor of the present invention can be formulated into any form and administered orally.

The administration method, dose and formulation method are shown below. i) Administration method The amylase inhibitor of the present invention can be administered orally, and is administered as soft / hard capsules or tablets, granules, fine granules, and powders. ii) Dosage The dose is not constant depending on the administration method, the malignancy of the disease, the age of the patient, the condition and general condition of the patient, the degree of progression of the disease, etc. 01-
500 g, for a dwarf it is usually 0.01-200 g. iii) Formulation method The proportion of the active ingredient of the amylase inhibitor of the present invention may be changed depending on the dosage form, but it is suitable to be approximately 0.3 to 15.0% by weight.

In the formulation of the amylase-inhibiting substance of the present invention, an aqueous solution, an oily formulation or the like may be prepared into a dosage form such as capsules, tablets and fine granules according to a conventional method, and then provided. it can. Further, in order to impart stability and acid resistance to the active ingredient for long-term storage and to completely maintain the medicinal effect, if a formulation with a further pharmaceutically acceptable film is prepared, excellent stability is obtained. It can be an amylase inhibitor.

The surfactants, excipients, lubricants, adjuvants, pharmaceutically acceptable film-forming substances and the like used in the formulation of the amylase inhibitor of the present invention are as follows. In order to improve the disintegration and elution of the inhibitor of the present invention, one or more surfactants such as alcohols, esters, polyethylene glycol derivatives, fatty acid esters of sorbitan, and sulfated fatty alcohols are used. It can be added.

As the excipient, for example, sucrose, lactose,
One or more of starch, crystalline cellulose, mannitol, light anhydrous silicic acid, magnesium aluminate, magnesium aluminometasilicate, synthetic aluminum silicate, calcium carbonate, sodium hydrogencarbonate, calcium hydrogenphosphate, carboxymethylcellulose calcium, etc. It can be added in combination.

As the lubricant, for example, magnesium stearate, talc, hydrogenated oil and the like can be added alone or in combination of two or more. As a flavoring agent and a flavoring agent, salt, saccharin, sugar, mannitol and orange are also added. Sweetening agents such as oil, licorice extract, citric acid, glucose, menthol, eucalyptus oil, malic acid, etc., flavors, coloring agents, preservatives and the like may be contained.

Examples of adjuvants such as suspending agents and wetting agents may include coconut oil, olive oil, sesame oil, peanut oil, calcium lactate, safflower oil, soybean phospholipid, and the like. As film-forming substances, cellulose acetate phthalate (CAP) is used as a carbohydrate derivative such as cellulose and saccharides, and methyl acrylate / methacrylic acid copolymer is used as a polyvinyl derivative such as acrylic acid copolymers and dibasic acid monoesters. Examples thereof include polymers and methyl methacrylate / methacrylic acid copolymers.

In addition, when coating the above film-forming substance, a coating aid which is usually used, for example, a plasticizer, and various additives for preventing mutual adhesion of the drugs during the coating operation are added to form the film. It can improve the properties of the agent and make the coating operation easier. Test Example (Assay for α-Amylase Inhibitory Activity) The bay leaves and deoiled bay leaves of the present invention were assayed for α-amylase inhibitory activity.

As the substrate solution, soluble starch (manufactured by Katayama Chemical Co., Ltd.) was added to 0.5% in 50 mM acetate buffer (pH 6.5).
Human saliva-derived α used as enzyme solution
-Amylase was used. Enzyme solution 5 to 0.25 ml of substrate solution
0 μl, assay solution 50 μl, 20 mM calcium chloride and 1
50 mM acetate buffer containing 00 mM sodium chloride (pH 6.
5) 50 μl and 50 mM acetate buffer (pH 6.5) 100 μl
l was added and the mixture was reacted at 37 ° C. for 15 minutes in a warm bath. After the reaction was completed, the mixture contained 1.7 mM potassium iodide and 0.17 mM iodine.
5 ml of 0017N hydrochloric acid aqueous solution was added, and the absorbance was measured at 700 nm.

The α-amylase inhibitory activity of bay leaves is 5
At 0% inhibitory concentration of 63 μg / ml, deoiled bay leaves are
It was g / ml. In addition, when the α-amylase inhibitory activity of a commercially available α-amylase inhibitor (manufactured by Sigma, derived from wheat germ) was assayed, the 50% inhibitory concentration was 229.5 μg.
/ Ml. The amylase inhibitor of the present invention can also be incorporated into food. Any type of food may be used, but in particular, a food containing a sugar such as starch is advantageous because the effect of the amylase inhibitor can be expected for the food. Examples of such foods include bread, noodles, biscuits, pancakes, dressings, drinks and the like.

When the amylase-inhibiting substance of the present invention is mixed in the food, the compounding amount is 0.001 to 100 with respect to the food.
It is preferably in the range of 0.01 to 30% by weight, especially 0.01 to 30% by weight.

[0019]

EXAMPLES The present invention will now be described in more detail with reference to examples. Example 1 1 kg of dried bay leaves [Sold by: Uchida Wakan Yaku Co., Ltd.]
Was immersed in 3 liters of hexane, left at room temperature for 24 hours, and then hexane was removed by filtration. Do this operation 3
Repeated times to deoil. The deoiled bay leaves were air dried for 1 day to produce 900 g of deoiled bay leaves.

Example 2 1 kg of laurel leaves was put in a container, and 5 liters of water was poured therein, and steam was introduced into the container for 1 hour to remove oil. Deoiled leaves are dried at 70 ° C with an air dryer or a hot air dryer.
600 g of dried and deoiled bay leaves were produced.

Example 3 Eggshell calcium 130 g, ascorbic acid 20 g, Avicel 40 g, sugar 285 g, deoiled bay leaf powder 25
g was mixed by a conventional method with a mixer and then tableted to produce tablet confectionery and tablets.

Example 4 (biscuits) Wheat flour 120 g, bay leaf powder 1.2 g, sugar 35 g, shortening 15 g, whole egg powder 1.5 g, salt 1 g, sodium hydrogen carbonate 0.6 g, ammonium carbonate 0.75 g, water 2
Using 0 g, a dough was prepared by a conventional method, molded and roasted to produce a biscuit.

Example 5 (Bread) Using 3 kg of wheat flour, 30 g of bay leaf powder, 60 g of yeast, 3 g of yeast food, 150 g of sugar, 60 g of salt, shortening 150 g, 60 g of skim milk powder, and 2070 g of water, a dough was prepared by a conventional method. Then, the bread was manufactured by molding and roasting.

Example 6 (noodles) A mixture of 1% by weight of bay leaf, 34% by weight of water, 1% by weight of salt and 1% by weight of starch was added to semi-strong wheat flour and kneaded for 12 minutes. Rolled and molded several times with a noodle machine to obtain raw noodle bands and raw noodle strings of Chinese noodles.

[0025]

INDUSTRIAL APPLICABILITY According to the present invention, there are provided an amylase inhibitor containing laurel leaves or deoiled laurel leaves as a main component and a food containing the same. The amylase inhibitor of the present invention has no problems in terms of safety and effectiveness, and has excellent activity.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (56) References Kiyochika Hoshikawa “Ingredients for Cooking and Confectionery 1 Spice” (Shibata Shoten 1977) pages 53–54

Claims (3)

[Claims] 1. An amylase inhibitor containing bay leaves as an active ingredient. 2. An amylase inhibitor containing deoiled bay leaves as an active ingredient. 3. A food containing the amylase inhibitor according to claim 1 or 2.