# US 2022/0030896 A2 · Choline ester-containing composition for oral ingestion

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- Number: US 2022/0030896 A2
- Document ID: US20220030896A2
- Status: Published application
- Kind: A2
- Application number: 16/341,748
- Filed: 2017-10-16
- Published: 2022-02-03
- Earliest claimed: 2016-10-14
- Assignees: Shinshu University
- Applicants: Shinshu University
- Inventors: KOZO NAKAMURA
- Web page: https://patentgrep.com/patent/US20220030896A2

## CPC

- A23L 33/105: Plant extracts, their artificial duplicates or their derivatives
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- A61K 31/221: with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
- A61K 36/81: Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
- A61K 36/899: Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61P 9/12: Antihypertensives
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

The object of the present invention is to provide a composition having a blood pressure-lowering effect and/or an anti-stress effect, wherein an active ingredient of a choline ester such as acetylcholine, and the like, can be easily administered to humans by the oral pathway. Consequently, the object of the present invention is to provide a novel composition for oral ingestion having a blood pressure-lowering effect and a vasodilatory effect, wherein a choline ester such as acetylcholine, and the like, can be easily administered to humans by the oral pathway, and to provide food which is a useful supply source therefore.

## Claims

### Claim 1

A composition having a blood pressure-lowering effect and/or an anti-stress effect and comprising a choline ester as an active ingredient, wherein the composition is for oral ingestion and wherein the choline ester content is 5 μg to 50 mg.

### Claim 2 (depends on 1)

The composition according to claim 1, wherein the composition is a food composition.

### Claim 3 (depends on 1)

The composition according to claim 1, wherein the composition is a pharmaceutical composition for lowering blood pressure and/or for anti-stress.

### Claim 4 (depends on 1, 2, 3)

The composition according to any one of claims 1 to 3, wherein the choline ester is derived from an edible plant.

### Claim 5 (depends on 1, 2, 3, 4)

The composition according to any one of claims 1 to 4, consisting of a lyophilized powder and/or a hot air-dried powder of edible plants.

### Claim 6 (depends on 5)

The composition according to claim 5, consisting of a lyophilized powder and/or a hot air-dried powder of edible plants, which can pass through a 20 mesh sieve.

### Claim 7 (depends on 1, 2, 3, 4)

The composition according to any one of claims 1 to 4, wherein the composition is an extract obtained by extracting edible plants with ethanol or hydrous ethanol.

### Claim 8 (depends on 4, 5, 6, 7)

The composition according to any one of claims 4 to 7, wherein the edible plant is a fruit of a Solanaceae Solanum eggplant species (Solanum melongena) and/or a young shoot of a bamboo subfamily of Piceaceae (Poaceae, Bambusoideae, Bambuseae).

### Claim 9 (depends on 1, 2, 3)

The composition according to any one of the claims 1 to 3, wherein the choline ester comprises one or more selected from the group consisting of acetylcholine, butyrylcholine and propionylcholine.

### Claim 10 (depends on 9)

The composition according to claim 9, wherein the choline ester does not contain lactoylcholine.

### Claim 11 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10)

The composition according to any one of claims 1 to 10, wherein the concentration of choline ester is 5 μg/g to 250 mg/g and the intake amount per day is adjusted from 5 μg to 50 mg.

### Claim 12 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11)

The composition according to any one of claims 1 to 11, wherein the composition is frozen.

### Claim 13 (depends on 1, 2, 3)

The composition according to any one of claims 1 to 3, wherein the composition is a part or the whole of the frozen fruit of a Solanaceae Solanum eggplant species (Solanum melongena).

### Claim 14

A method of producing a composition for oral ingestion having a blood pressure-lowering effect and/or an anti-stress effect and comprising a choline ester as an active ingredient, wherein the method comprises
a step for making an edible plant into a lyophilized powder and/or a hot air-dried powder, and
a step for dispensing the lyophilized powder and/or the hot air-dried powder so that the choline ester content is 5 μg to 50 mg.

### Claim 15 (depends on 14)

The method according to claim 14, wherein the edible plant is a fruit of a Solanaceae Solanum eggplant species (Solanum melongena) and/or a young shoot of a bamboo subfamily of Piceaceae (Poaceae, Bambusoideae, Bambuseae).

### Claim 16 (depends on 14, 15)

The method according to claim 14 or 15, wherein the method further comprises
a step for heating the edible plant.

### Claim 17 (depends on 14, 15, 16)

The method according to any one of claims 14 to 16, wherein the method further comprises
a step for suspending the lyophilized powder and/or a hot air-dried powder of an edible plant in water, and a step for adding an acid to the suspension obtained.

### Claim 18 (depends on 17)

The method according to claim 17, wherein the method further comprises
a step for adjusting the suspension to which acid has been added to a pH of 5.5 to 4.5.

### Claim 19 (depends on 14, 15, 16, 17, 18)

A composition for oral ingestion having a blood pressure-lowering effect and/or an anti-stress effect and comprising a choline ester as an active ingredient, which is produced by a method according to any one of claims 14 to 18.

### Claim 20

A method for producing an extract for oral ingestion having a blood pressure-lowering effect and/or an anti-stress effect and comprising a choline ester as an active ingredient, wherein the method comprises
a step for extracting an edible plant or a lyophilized powder and/or a hot air-dried powder of an edible plant with ethanol or hydrous ethanol.

### Claim 21 (depends on 20)

The method according to claim 20, wherein the method comprises
a step for extracting an edible plant or a lyophilized powder and/or hot air-dried powder of an edible plant with ethanol.

### Claim 22 (depends on 20)

The method according to claim 20, wherein the method comprises
a step for extracting an edible plant or a lyophilized powder and/or a hot air-dried powder of an edible plant with ethanol, and wherein the ethanol concentration of the hydrous ethanol is 25 to 60% (w/w), or 95% (w/w) or more.

### Claim 23 (depends on 20, 21, 22)

The method according to any one of claims 20 to 22, wherein L-ascorbic acid is added to the ethanol or the hydrous ethanol used for the extraction.

### Claim 24 (depends on 20, 21, 22, 23)

The method according to any one claims 20 to 23, wherein the method comprises
a step for adjusting the choline ester content of the extract from 5 μg to 50 mg.

### Claim 25 (depends on 20, 21, 22, 23, 24)

An extract for oral ingestion having a blood pressure-lowering effect and/or an anti-stress effect and comprising a choline ester as an active ingredient produced according to any one of claims 20 to 24.
