# US 2015/0209338 A1 · Method for decreasing symptoms of alcohol consumption

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- Number: US 2015/0209338 A1
- Document ID: US20150209338A1
- Status: Published application
- Kind: A1
- Application number: 14/678,502
- Filed: 2015-04-03
- Published: 2015-07-30
- Earliest claimed: 2007-07-03
- Assignees: Alcobra Ltd.
- Applicants: Alcobra Ltd.
- Inventors: Gur Megiddo; Dalia Megiddo; Rina Yamin; Yaron Ilan; Shimon Amselem
- Web page: https://patentgrep.com/patent/US20150209338A1

## CPC

- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 9/0007: {Effervescent (A61K9/0065 takes precedence)}
- 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 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/5026: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/7061: {Polyacrylates}
- A61K 31/4015: having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
- A61K 31/4415: Pyridoxine, i.e. Vitamin B6 (pyridoxal phosphate A61K31/675)
- A61K 31/455: Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/30: for treating abuse or dependence
- A61P 25/32: Alcohol-abuse
- A61P 39/00: General protective or antinoxious agents
- A61P 39/02: Antidotes
- 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

## Abstract

The present invention relates to methods and compositions of metadoxine and physiologically compatible active derivatives thereof, and their use for decreasing symptoms of alcohol consumption as well as in the prevention of alcohol consumption related symptoms in subjects in need thereof.

## Claims

### Claim 1

A method for decreasing or preventing symptoms or effects of alcohol consumption in a subject in need thereof, wherein said subject has not reached intoxication, comprising non-chronic administration of a composition comprising metadoxine.

### Claim 2

A method for preventing alcohol intoxication in a subject in need thereof, wherein said subject has not reached intoxication, comprising administering a composition comprising metadoxine.

### Claim 3

A method for reducing or eliminating blood alcohol levels in a subject in need thereof, wherein said subject has not reached intoxication, comprising administering a composition comprising metadoxine.

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

The method according to claim 2 or 3, wherein said composition is administered by non-chronic administration.

### Claim 5

The method according to any one of the preceding claims, wherein said subject is or will be social drinking, session drinking or binge drinking.

### Claim 6

The method according to any one of the preceding claims, wherein said composition is administered in a single dosage form or portion thereof.

### Claim 7

The method of any one of the preceding claims, wherein the mode of administration is oral, sublingual, buccal, nasal, transdermal, transmucosal, rectal or subcutaneous administration.

### Claim 8

A composition comprising metadoxine formulated for sustained or controlled release upon administration to a subject.

### Claim 9

A composition comprising metadoxine, wherein a portion of the metadoxine is formulated for sustained release and a portion of the metadoxine is formulated for immediate release upon administration to a subject.

### Claim 10 (depends on 8)

The composition according to claim 8, wherein the relative proportion of sustained release metadoxine to immediate release metadoxine is in a range of from 1-to-99 to 99-to-1, in whole integers.

### Claim 11 (depends on 8, 9, 10)

The composition according to any one of claims 8-10, selected from a pharmaceutical composition, a dietary supplement, a food and a beverage.

### Claim 12 (depends on 8, 9, 10, 11)

The composition according to any one of claims 8-11, wherein said metadoxine is a physiologically compatible derivative.

### Claim 13 (depends on 8, 9, 10, 11, 12)

The composition according to any one of claims 8-12, wherein said composition is formulated for non-chronic administration.

### Claim 14 (depends on 13)

The composition according to claim 13, wherein said composition is administered in a single dosage form or portion thereof.

### Claim 15 (depends on 8, 9, 10, 11, 12, 13, 14)

The composition according to any one of claims 8-14, wherein said composition is formulated to release not less than 50% of the total metadoxine within 8 hours.

### Claim 16 (depends on 8, 9, 10, 11, 12, 13, 14)

The composition according to any one of claims 8-14, wherein said composition is formulated to release not less than 50% of the total metadoxine within 6 hours.

### Claim 17 (depends on 8, 9, 10, 11, 12, 13, 14)

The composition according to any one of claims 8-14, wherein said composition has a tmax of metadoxine in the blood greater than about 1 hour.

### Claim 18 (depends on 17)

The composition according to claim 17, wherein said composition has a tmax of metadoxine in the blood that is about 2-fold greater than in an immediate release composition.

### Claim 19 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)

The composition according to any one of claims 8-18, wherein said composition is formulated to deliver up to 3000 mg of metadoxine in a single dose administration or portion thereof.

### Claim 20 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19)

The composition according to any one of claims 8-19, wherein said composition further comprises a polymeric material.

### Claim 21 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)

The composition according to any one of claims 8-20, wherein said composition further comprises an absorption enhancer.

### Claim 22 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21)

The composition according to any one of claims 8-21, wherein said composition further comprises an acceptable excipient.

### Claim 23 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22)

The composition according to any one of claims 8-22, wherein said composition comprises or consists essentially of Formula 1.

### Claim 24 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22)

The composition according to any one of claims 8-22, wherein said composition comprises or consists essentially of Formula 2.

### Claim 25 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22)

The composition according to any one of claims 8-22, wherein said composition comprises or consists essentially of Formula 3.

### Claim 26 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25)

The composition according to any one of claims 8-25, wherein said sustained release is controlled release.

### Claim 27 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26)

A method for increasing the mean tmax of metadoxine in the blood of a subject in need thereof comprising administering a composition according to any one of claims 8-26.

### Claim 28 (depends on 27)

The method according to claim 27, wherein said composition has a tmax of metadoxine in the blood that is about 2-fold greater than in an immediate release composition.

### Claim 29 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26)

The method according to any one of claims 1-7, wherein said composition is a composition according to any one of claims 8-26.

### Claim 30 (depends on 28, 29)

The method according to any one of claims 28-29, wherein said subject is or will be social drinking, session drinking or binge drinking.

### Claim 31 (depends on 28, 29, 30)

The method according to any one of claims 28-30, wherein said composition is administered by non-chronic administration.

### Claim 32 (depends on 31)

The method according to claim 31, wherein said composition is administered in a single dosage form or portion thereof.

### Claim 33 (depends on 28, 29, 30, 31, 32)

The method of any one of claims 28-32, wherein said mode of administration is oral, nasal, rectal, subcutaneous, transmucosal, sublingual, buccal or transdermal administration.

### Claim 34

Use of metadoxine or a functional derivative thereof in the manufacture of a therapeutic composition for reducing or eliminating blood alcohol level.

### Claim 35

Use of metadoxine or a functional derivative thereof in the manufacture of a therapeutic composition for decreasing or preventing symptoms or effects of alcohol consumption.

### Claim 36

Use of metadoxine or a functional derivative thereof in the manufacture of a therapeutic composition for preventing alcohol intoxication.

### Claim 37

Use of metadoxine or a functional derivative thereof formulated for sustained or controlled release in the manufacture of a therapeutic composition for increasing the mean tmax of metadoxine in the blood.

### Claim 38 (depends on 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26)

A drug delivery device comprising a metadoxine composition according to any one of claims 8-26.