JP6940109B2 - Composition for improving cognitive function in dementia - Google Patents

Description

The present invention relates to a composition for improving brain function.

With the advent of an aging society in recent years, the decline in brain function caused by degenerative diseases of the elderly's brain, especially Alzheimer's disease, Lewy body dementia, Parkinson's disease, etc., is becoming a widespread problem.

Since dementia caused by such degenerative diseases of the brain may lead to serious situations that threaten even human dignity, research on prevention and treatment of dementia has been energetically promoted in recent years. Has been done.

While studying risk factors that cause dementia, the present inventor tried to put into practical use a composition having a simple and effective effect of improving brain function by combining supplement-like safe ingredients, and Patent Document 1 In the present invention, it has been found that a composition obtained by mixing a predetermined silicic acid derivative compound and coral calcium powder in a predetermined ratio is useful for improving brain function.

WO 2015/016285

An object of the present invention is to find a new therapeutic method for dementia, and specifically, to make the brain function improving action in the composition composed of the main components shown in Patent Document 1 more effective. That is.

The present inventor has already discovered that homocysteine acid (HCA), which is an oxidant of methionine, is involved as one of the risk factors in the onset of Alzheimer's disease, and the binding of HCA to the NMDA receptor. Patent Document 1 has been filed for an invention targeting inhibition. This time, as a result of further various studies on HCA, while investigating means for lowering the concentration of HCA in the body, we focused on promoting its metabolism and examined various metabolic enzymes and substances that activate the enzymes. However, it was discovered that a nicotinic acid amide derivative that activates glutamate dehydrogenase has a brain function improving effect, and further, by adding a nicotinic acid amide derivative to a mixture of coral calcium and a carcinic acid derivative compound, a brain function improving effect can be obtained. It has been found that the present invention is remarkably improved, and the present invention has been completed.

The present invention includes the following aspects.
[Item 1] A composition for improving brain function containing coral calcium, a cinnamic acid derivative compound, and a nicotinamide derivative.

[Item 2] The composition of Item 1, wherein the cinnamic acid derivative is selected from ferulic acid, caffeic acid, and / or sinapic acid.

[Item 3] The composition of Item 1, wherein the cinnamic acid derivative is ferulic acid.

[Item 4] The composition according to any one of Items 1 to 3, wherein the nicotinamide derivative is nicotinamide, niacin, or NAD.

[Item 5] The composition according to any one of Items 1 to 3, wherein the nicotinamide derivative is NAD.

[Item 6] The composition according to any one of Items 1 to 3, wherein the nicotinamide derivative is niacin.

[Item 7] The composition according to any one of Items 1 to 6, which contains 1.5 to 3 parts by weight of the cinnamic acid derivative and 1 to 2 parts by weight of the nicotinamide derivative with respect to 1 part by weight of coral calcium. ..

[Item 8] The composition according to any one of Items 1 to 7, further containing ascorbic acid and / or lycopene.

[Item 9] The composition according to any one of Items 1 to 8, further containing matcha powder, cocoa powder, hydroxysilica powder, and / or dried Japanese ginseng powder.

[Item 10] A supplement containing the composition according to any one of Items 1 to 9.

[Item 11] A brain function improving agent containing the composition according to any one of Items 1 to 9.

[Item 12] A method for improving brain function, which comprises administering a therapeutically effective amount of a combination of coral calcium, a cerebral acid derivative compound, and a nicotinamide derivative to a patient in need of treatment.

[Item 13] Use of a combination of coral calcium, a cinnamic acid derivative compound, and a nicotinamide derivative for producing a brain function improving agent.

[Item 14] A composition for improving brain function containing a nicotinamide derivative.

In the present invention, as described in Patent Document 1, to the NMDA receptor associated with an increase in the concentration of homocysteine acid, which is considered as one of the pathogenic mechanisms of neurodegenerative diseases such as Alzheimer's disease, Levy body dementia, and Parkinson's disease. The excess binding of Parkinson's disease is inhibited by the effect of the combination of coral calcium and diatomic acid derivative compound to exert improvement in brain function, and by adding a new nicotinic acid amide derivative, the improvement in brain function is further significantly improved. Can be expected.

Coral calcium is a substance made from fossil coral, which is usually used as a powder and is commercially available as a health food as a source of marine minerals mainly composed of calcium and magnesium. Further, it is said that the coral calcium powder contains calcium hydride at a ratio of about 5%, and it is widely used as a hydrogen supplement capable of ingesting active hydrogen from this calcium hydride. In general chemical terms, calcium hydride _{means CaH 2} that reacts violently with water, but the calcium hydride in the coral calcium powder here is different from this, and is a carbon dioxide having an active hydrogen compound adsorbed. It means calcium and is a term widely used in the field of health supplements.

更に具体的には、上記Ｒ１がメトキシ基、Ｒ２が水酸基、Ｒ３が水素のフェラル酸、Ｒ１とＲ２が水酸基、Ｒ３が水素のコーヒー酸、Ｒ１とＲ３がメトキシ基、Ｒ２が水酸基のシナピン酸が挙げられる。The silicate acid derivative compound is a derivative of silicate acid mainly by introducing a substituent into the benzene ring portion, for example, silicate acid having 1 to 3 hydroxyl groups or alkoxy groups on the benzene ring. Specifically, it is a compound having the following structure.

More specifically, the above-mentioned R1 is a methoxy group, R2 is a hydroxyl group, R3 is a hydrogen ferral acid, R1 and R2 are hydroxyl groups, R3 is hydrogen caffeic acid, R1 and R3 are methoxy groups, and R2 is a hydroxyl group. Can be mentioned.

The nicotinamide derivative is a nicotinamide or a compound containing a nicotinamide structure, which is a general term for compounds used in pharmaceuticals, foods and the like, and examples thereof include nicotinamide dinucleotide (NAD) and niacin.
The niacin is a generic name for nicotinic acid and nicotinamide, which may also be referred to as vitamin B _3.
Nicotinamide adenine dinucleotide (NAD) is known as a coenzyme involved in energy metabolism having the following structure, and is also used as a supplement.

The amount of coral calcium used in the present invention is not particularly limited as long as it is determined in consideration of the amount of calcium normally ingested by humans, but is 50 to 3000 mg, preferably 100 to 300 mg, and more preferably 150 to 250 mg per day. ..

The amount of the cinnamic acid derivative compound used in the present invention is not particularly limited as long as it is normally ingested by humans, but is 300 to 700 mg, preferably 400 to 600 mg, and more preferably 500 to 600 mg per day. The mixing ratio with coral calcium is 1 to 4 parts by weight, preferably 1.5 to 3 parts by weight, more preferably 1.5 to 2.5 parts by weight, based on 1 part by weight of coral calcium. Is.

The amount of the nicotinic acid amide derivative used in the present invention is not particularly limited as long as it is normally ingested by humans, but is 50 to 300 mg, preferably 100 to 300 mg, and more preferably 200 to 300 mg per day. The mixing ratio with coral calcium is 0.5 to 3 parts by weight, preferably 1 to 2 parts by weight, and more preferably 1 to 1.5 parts by weight of the nicotinamide derivative with respect to 1 part by weight of coral calcium. ..

In the present invention, the effect of the present invention can be promoted by adding ascorbic acid, lycopene and the like to a mixture of coral calcium, a cinnamic acid derivative compound, and NAD. In the case of ascorbic acid, the amount to be added is 1 to 3 parts by weight, preferably 1.5 to 2.5 parts by weight, and more preferably 1.8 to 2.2 parts by weight with respect to 1 part by weight of coral calcium. In the case of lycopene, it is 1 to 2 parts by weight, preferably 1.2 to 1.5 parts by weight, and more preferably 1.3 to 1.5 parts by weight with respect to 1 part by weight of coral calcium.

Further, in the present invention, matcha powder, cocoa powder, hydroxysilica powder, dried Japanese mountain ginseng powder and the like may be further added for the purpose of adding flavor, and these components may promote the effect of improving brain function. You can expect it. The amount of these components added is 1 to 6 parts by weight of matcha powder and cocoa powder, 0.5 to 2 parts by weight of hydroxysilica powder, and 0.1 to 0 parts by weight of dried Nihonyama ginseng powder with respect to 1 part by weight of coral calcium. .5 parts by weight.

The composition of the present invention may be taken once or several times a day, specifically, once, twice, three times, four times a day or the like.

In the present invention, improvement of brain function means improvement for degenerative diseases of the brain, and specifically includes improvement for neurodegenerative diseases such as dementia, Alzheimer's disease, Levy body dementia, and Parkinson's disease.
The composition for improving brain function of the present invention antagonizes and inhibits the binding of homocysteine acid to the NMDA receptor to prevent cell damage. In addition, the composition for improving brain function of the present invention is widely effective for diseases diagnosed as brain dysfunction such as dementia by MMSE (Mini-Mental State Examination).

The composition for improving brain function of the present invention can also be used as a supplement or a raw material thereof, and as a brain function improving agent or a raw material thereof.

The composition for improving brain function according to the present embodiment may be used as it is as a mixed powder, or may be used as a pharmaceutical product prepared by adding a commonly used pharmaceutical component. Dosage forms include tablets, capsules, granules and powders. In the case of tablets and granules, they may be coated by a well-known method. The pharmaceutical product is produced by a known method using pharmaceutically acceptable additives.

Additives include excipients, disintegrants, binders, fluidizers, lubricants, coatings, solubilizers, solubilizers, thickeners, dispersants, stabilizers, and sweeteners, depending on the purpose. , Perfume and the like can be used. Specifically, for example, lactose, mannitol, crystalline cellulose, low-substituted hydroxypropyl cellulose, corn starch, partially pregelatinized starch, carmellose calcium, croscarmellose sodium, hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyvinyl alcohol, stearer. Examples thereof include magnesium acid, stearyl sodium fumarate, polyethylene glycol, propylene glycol, titanium oxide, and talc.

When the compound of the present invention is prepared in a single preparation, for example, the composition of the mixture of the present invention may be contained in an amount of 0.1 to 70% by weight based on the total composition of the preparation.

Hereinafter, the present invention will be described in more detail with reference to Examples, but the present invention is not limited thereto.

Example 1 (Effect test of NAD addition)
(Test method)
Five subjects were given the mixture shown in the table below twice a day, and after 2 months, the cognitive function test MMSE was performed.

(result)
The table below shows the results before the start of the test and the results after 2 months. All subjects showed improvement in cognitive function.

Test 2. (Comparative test with / without niacin added)
A comparative experiment was conducted to determine whether the addition of niacin further improves the effects of coral calcium and cinnamic acid derivative compounds on improving brain function.
(Test method)
Six subjects admitted to the same care facility were divided into two groups of three each, with the mixture of the formulations shown in the table below in one group and the mixture of the formulations in the table below without niacin in the other group. The drug was taken once a day, and after one month, the cognitive function test MMSE was performed.

(result)
The table below shows the results after one month, as well as the results before the start of the test. The MMSE was unchanged or slightly reduced in the niacin-free formulation group. On the other hand, in the group to which the prescription containing niacin was administered, MMSE was increased and cognitive function was improved.

Claims (9)

Coral calcium, cinnamic acid derived body, and contains a nicotinamide derivative,
The nicotinamide derivative is niacin or NAD,
Cinnamic acid derivatives are selected from ferulic acid, caffeic acid, and / or sinapic acid,
It contains 1 to 4 parts by weight of a ceramic acid derivative and 0.5 to 3 parts by weight of a nicotinamide derivative with respect to 1 part by weight of coral calcium.
Oral composition for improving brain function related to dementia. The composition of claim 1, wherein the cinnamic acid derivative is ferulic acid. The composition of claim 1 or 2 , wherein the nicotinamide derivative is NAD. The composition of claim 1 or 2 , wherein the nicotinamide derivative is niacin. The composition according to any one of claims 1 to 4 , wherein the cinnamic acid derivative is contained in a ratio of 1.5 to 3 parts by weight and the nicotinamide derivative is contained in a ratio of 1 to 2 parts by weight with respect to 1 part by weight of coral calcium. The composition according to any one of claims 1 to 5 , further containing ascorbic acid and / or lycopene. The composition according to any one of claims 1 to 6 , further containing matcha powder, cocoa powder, hydroxysilica powder, and / or dried Japanese ginseng powder. A supplement containing the composition according to any one of claims 1 to 7. A brain function improving agent for dementia containing the composition according to any one of claims 1 to 7.