# US 9,040,063 B2 · Orally administrable gallium compositions and methods of use

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- Number: US 9,040,063 B2
- Document ID: US9040063B2
- Status: Granted
- Kind: B2
- Application number: 14/036,576
- Filed: 2013-09-25
- Published: 2014-01-23
- Granted: 2015-05-26
- Earliest claimed: 2005-10-27
- Applicants: Lawrence Richard Bernstein
- Inventors: Lawrence Richard Bernstein
- Web page: https://patentgrep.com/patent/US9040063B2

## CPC

- A61K 47/38: Cellulose; Derivatives thereof
- A23K 20/20: Inorganic substances, e.g. oligoelements
- A23L 33/16: Inorganic salts, minerals or trace elements
- 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 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/4858: {Organic compounds}
- A61K 9/4866: {Organic macromolecular compounds}
- A61K 31/28: Compounds containing heavy metals
- A61K 31/555: containing heavy metals, e.g. hemin, hematin, melarsoprol
- A61K 31/717: Celluloses
- A61K 33/24: Heavy metals; Compounds thereof
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 31/04: Antibacterial agents
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A61K 33/242: Gold; Compounds thereof
- A61K 33/243: Platinum; Compounds thereof
- A61K 33/244: Lanthanides; Compounds thereof (medicinal preparations containing radioactive lanthanides for use in therapy or testing in vivo A61K51/00)
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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)
- A23K: FODDER
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

Provided are pharmaceutical gallium compositions that are particularly useful for oral administration. The pharmaceutical compositions include solid, liquid, and paste formulations, which have high oral gallium bioavailability and are suitable for human and veterinary applications. The compositions comprise pharmaceutically acceptable gallium compounds, such as gallium maltolate, gallium 8-quinolinolonate, or gallium nitrate, together with certain viscosity-increasing agents, such as water-soluble forms of methylcellulose or carboxymethylcellulose.

## Claims

### Claim 1

A method for increasing the oral bioavailability of gallium from an orally administered gallium compound, the increase being relative to the oral bioavailability of gallium from the gallium compound when it is orally administered without a pharmaceutically acceptable viscosity-increasing agent, comprising the administration to a human or veterinary subject of a pharmaceutical composition comprising a pharmaceutically acceptable gallium compound and a pharmaceutically acceptable viscosity-increasing agent, wherein said gallium compound is not gallium 8-quinolinolate and the viscosity-increasing agent is water-soluble and not a cross-linked form of carboxymethylcellulose or povidone, and wherein the pharmaceutical composition comprises a viscous liquid or paste.

### Claim 2 (depends on 1)

The method of claim 1, wherein the viscosity-increasing agent is selected from the group consisting of viscosity-increasing forms of methylcellulose, carboxymethylcellulose, hydroxypropyl methylcellulose, and other water-soluble cellulose derivatives.

### Claim 3 (depends on 2)

The method of claim 2, wherein the viscosity-increasing agent is a viscosity-increasing form of methylcellulose or carboxymethylcellulose.

### Claim 4 (depends on 3)

The method of claim 3, wherein the viscosity-increasing agent is a viscosity-increasing form of carboxymethylcellulose.

### Claim 5 (depends on 1)

The method of claim 1, wherein the gallium compound is selected from the group consisting of gallium nitrate, gallium sulfate, gallium chloride, gallium citrate, gallium acetate, gallium tartrate, gallium gluconate, gallium palmitate, gallium succinate, gallium maltolate, gallium ethyl maltolate, gallium pyridinones, gallium protoporphyrin IX, gallium pyridoxal isonicotinoyl hydrazone, and bis(2-acetylpyridine 4N-dimethylthiosemicarbazone) gallium(III), gallium(III) tetrachloride.

### Claim 6 (depends on 5)

The method of claim 5, wherein the gallium compound is gallium maltolate.

### Claim 7 (depends on 1)

The method of claim 1, wherein the weight ratio of the gallium compound to the viscosity-increasing agent is approximately 0.1 to 1000.

### Claim 8 (depends on 7)

The method of claim 7, wherein the weight ratio of the gallium compound to the viscosity-increasing agent is approximately 1 to 500.

### Claim 9 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition comprises gallium maltolate, non-cross-linked carboxymethylcellulose, benzyl alcohol, water, and simple syrup.

### Claim 10 (depends on 9)

The method of claim 9, wherein the pharmaceutical composition comprises 1 to 20% w/v gallium maltolate, 10 to 30% v/v simple syrup, 0.1 to 4% v/v benzyl alcohol, 0.5 to 2.5% w/v non-cross-linked carboxymethylcellulose, and a balance of water.

### Claim 11 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition further comprises animal feed.

### Claim 12 (depends on 8)

The method of claim 8, wherein the weight ratio of the gallium compound to the viscosity-increasing agent is approximately 1 to 250.

### Claim 13 (depends on 12)

The method of claim 12, wherein the weight ratio of the gallium compound to the viscosity-increasing agent is approximately 10 to 100.