# US 10,245,278 B2 · Liquid or semi-liquid pharmaceutical, dietary or food composition free of bitterness containing an arginine salt

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- Number: US 10,245,278 B2
- Document ID: US10245278B2
- Status: Granted
- Kind: B2
- Application number: 14/787,924
- Filed: 2014-04-30
- Published: 2016-03-31
- Granted: 2019-04-02
- Earliest claimed: 2013-05-02
- Applicants: Philippe Gorny
- Inventors: Philippe Gorny
- Web page: https://patentgrep.com/patent/US10245278B2

## CPC

- A61K 31/7028: Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A23L 2/52: Adding ingredients (adding preservatives A23B70/10)
- A23L 2/56: Flavouring or bittering agents (sweeteners A23L2/60)
- A23L 2/60: Sweeteners
- A23L 27/34: {Sugar alcohols}
- A23L 27/84: {Flavour masking or reducing agents}
- A23L 29/35: {Degradation products of starch, e.g. hydrolysates, dextrins; Enzymatically modified starches}
- A23L 33/10: using additives (addition of substantially indigestible substances A23L33/21)
- A23L 33/17: Amino acids, peptides or proteins
- A23L 33/175: Amino acids
- A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 31/375: Ascorbic acid, i.e. vitamin C; Salts thereof
- A61K 31/522: having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
- A61K 31/616: by carboxylic acids, e.g. acetylsalicylic acid
- A61K 36/258: Panax (ginseng)
- A61K 36/77: Sapindaceae (Soapberry family), e.g. lychee or soapberry
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 3/02: Nutrients, e.g. vitamins, minerals
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 37/04: Immunostimulants
- A61P 39/06: Free radical scavengers or antioxidants
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- 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)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- 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

An aqueous, liquid or semi-liquid pharmaceutical or dietary composition, including at least one L-arginine salt on the basis of at least one gram of the salt per dosage unit. Adding the quantity of water necessary to dissolve an arginine salt, maltitol and, optionally, an alcohol or an alcoholate, ensures the removal of the bitterness from the liquid or semi-liquid compositions made from salified arginine. This specific composition allows considerable doses of arginine to be taken directly via oral administration, by drinking, without adding additional water. Also, a food composition containing a dietary composition as defined above.

## Claims

### Claim 1

A liquid or semi-liquid, aqueous dietary or pharmaceutical composition, comprising at least one salt of L-arginine in an amount of at least one gram of said salt per unit dose, said composition comprising
maltitol, in an amount of 1 to 1.5 times the weight of said arginine salt in the composition,
water, in an amount of 1.5 to 3 times the weight of said arginine salt in the composition, and
an alcohol or an alcoholate.

### Claim 2

A liquid or semi-liquid, aqueous dietary, pharmaceutical composition, comprising at least one salt of L-arginine in an amount of at least one gram of said salt per unit dose, said composition comprising:
from 15 to 30% by weight of L-arginine salt,
from 15 to 45% by weight of maltitol, and
from 0.1% to 12% by weight of an alcohol or of an alcoholate, relative to the total weight of the composition.

### Claim 3 (depends on 1)

A composition according to claim 1, characterized in that it is a pharmaceutical composition.

### Claim 4 (depends on 1)

A composition according to claim 1, characterized in that it is a dietary composition.

### Claim 5 (depends on 1)

A composition according to claim 1, wherein the alcohol or the alcoholate is present in an amount of from 0.1% to 12% by weight, relative to the total weight of the composition.

### Claim 6 (depends on 1)

A composition according to claim 1, comprising a single salt of L-arginine.

### Claim 7 (depends on 1)

A composition according to claim 1, comprising a weight of water equal to a 1.8 times to 2.5 times the weight of arginine salt of the composition or a weight of water comprised anywhere between these two limits.

### Claim 8 (depends on 1)

A composition according to claim 1, further comprising at least one strong sweetener.

### Claim 9 (depends on 8)

A composition according to claim 8, wherein said strong sweetener is sucralose and/or aspartame.

### Claim 10 (depends on 9)

A composition according to claim 9, wherein the strong sweetener(s) is (are) present in an amount, respectively, of from 0.01% to 1% by weight, relative to the total weight of the composition.

### Claim 11 (depends on 1)

A composition according to claim 1, further comprising at least one preservative additive and/or at least one antioxidant.

### Claim 12 (depends on 11)

A composition according to claim 11, wherein the preservative additive is chosen from potassium sorbate, sorbic acid, or mixtures thereof, and the antioxidant is ascorbic acid.

### Claim 13 (depends on 1)

A composition according to claim 1, comprising at least one L-arginine salt in an amount of one to ten grams per unit dose.

### Claim 14 (depends on 1)

A composition according to claim 1, wherein the arginine salt is chosen from arginine aspartate, arginine hydrochloride, arginine glutamate, arginine pyroglutamate, arginine pidolate, arginine ketoglutarate, or mixtures of these.

### Claim 15 (depends on 1)

A composition according to claim 1, further comprising at least one purine.

### Claim 16 (depends on 1)

A composition according to claim 1, further comprising at least one mineral component or a salt thereof.

### Claim 17 (depends on 1)

A composition according to claim 1, characterized in that it also comprises at least one amino acid other than arginine, or a metabolite of said amino acid or a salt thereof.

### Claim 18 (depends on 17)

A composition according to claim 17, wherein said amino acid other than arginine is chosen from lysine, cystine, cysteine, N-acetyl-cysteine and S-adenosylmethionine or one of their salts.

### Claim 19 (depends on 1)

A composition according to claim 1, further comprising at least one active ingredient other than a salt of L-arginine chosen from cafeine, guarana, maca, a vitamin, and acetylsalicylic acid.

### Claim 20 (depends on 1)

A composition according to claim 1, characterized in that it is in a form which may be administered orally or sublingually, in liquid, semi-liquid form or a lyophilized form prepared from a liquid or semi-liquid composition.

### Claim 21 (depends on 4)

A liquid or semi-liquid food composition containing at least one dietary composition according to claim 4.

### Claim 22 (depends on 1)

A method for the treatment of disorders of the physiological and/or anatomical response to sexual stimulation in humans, comprising administering to a subject in need thereof an effective amount of a pharmaceutical or dietary composition according to claim 1.

### Claim 23 (depends on 1)

A method for the treatment of the cardiovascular disorders in which a relaxation of the smooth muscle fibers of the heart and vessels is desired or provides benefit, comprising administering to a subject in need thereof an effective amount of a pharmaceutical or dietary composition according to claim 1.

### Claim 24 (depends on 1)

A method for the treatment of the cardiovascular disorders due to or associated with dysfunction of the vascular endothelial cells, comprising administering to a subject in need thereof an effective amount of a pharmaceutical or dietary composition according to claim 1.

### Claim 25 (depends on 1)

A method for the stimulation of growth hormone or the acceleration of the wound healing processes, or in the treatment of states of fatigue, comprising administering to a subject in need thereof an effective amount of a pharmaceutical or dietary composition according to claim 1.

### Claim 26 (depends on 1)

A method for the treatment of a reduction in immunity comprising administering to a subject in need thereof an effective amount of a pharmaceutical or dietary composition according to claim 1.

### Claim 27

A method of masking the bitterness of salified arginine in a food, dietary or pharmaceutical composition, comprising mixing maltitol, and an alcohol or an alcoholate with said salified arginine in a food, dietary or pharmaceutical composition, wherein the amount of maltitol in the combined composition is 1 to 1.5 times the amount of arginine by weight, and the amount of water in the combined composition is 1.5 to 3 times the amount of arginine by weight.

### Claim 28

A liquid or semi-liquid, aqueous dietary, pharmaceutical composition, comprising at least one salt of L-arginine in an amount of at least one gram of said salt per unit dose, said composition comprising:
from 20 to 30% by weight of L-arginine salt,
from 20 to 40% by weight of maltitol, and
from 0.1% to 12% by weight of an alcohol or of an alcoholate, relative to the total weight of the composition.

### Claim 29 (depends on 1)

A composition according to claim 1, wherein the alcohol or the alcoholate is present in an amount of from 1% to 5% by weight, relative to the total weight of the composition.

### Claim 30 (depends on 9)

A composition according to claim 9, wherein the strong sweetener(s) is (are) present in an amount, respectively, of from 0.01% to 0.5% by weight, relative to the total weight of the composition.

### Claim 31 (depends on 1)

A composition according to claim 1, comprising at least one L-arginine salt in an amount of 5 grams or 8 grams per unit dose.

### Claim 32 (depends on 1)

A composition according to claim 1, further comprising adenosine monophosphate (AMP).

### Claim 33 (depends on 1)

A composition according to claim 1, further comprising magnesium, potassium or one of their salts.

### Claim 34 (depends on 23)

A method according to claim 23, wheriein the cardiovascular disorders in which a relaxation of the smooth muscle fibers of the heart and vessels is desired or provides benefit are selected from the group consisting of high blood pressure, arteritis of the lower limbs, heart failure and ischemic heart diseases.

### Claim 35 (depends on 24)

A method according to claim 24, wherein the cardiovascular disorders due to or associated with dysfunction of the vascular endothelial cells are selected from the group consisting of atherosclerosis and/or diabetes and the disorders affected by age or tabacco addiction.
