# US 10,945,974 B2 · Methods and compositions to modulate the gut microbiota and to manage weight

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- Number: US 10,945,974 B2
- Document ID: US10945974B2
- Status: Granted
- Kind: B2
- Application number: 15/575,942
- Filed: 2016-05-31
- Published: 2018-05-31
- Granted: 2021-03-16
- Earliest claimed: 2015-06-01
- Assignees: Xeno Biosciences Inc.
- Applicants: Xeno Biosciences Inc.
- Inventors: Hasan Celiker
- Web page: https://patentgrep.com/patent/US10945974B2

## CPC

- A61K 31/17: having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine (isoureas, isothioureas A61K31/155; sulfonylureas A61K31/64)
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/2846: {Poly(meth)acrylates}
- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/4866: {Organic macromolecular compounds}
- A61K 9/4891: {Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004)}
- A61K 31/185: Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids (hydroxamic acids A61K31/16; peroxy acids A61K31/327)
- A61K 31/327: Peroxy compounds, e.g. hydroperoxides, peroxides, peroxyacids
- A61K 33/00: Medicinal preparations containing inorganic active ingredients
- A61K 33/40: Peroxides
- A61K 38/44: Oxidoreductases (1)
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- C12Y 111/01006: Catalase (1.11.1.6)
- 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
- C12Y: ENZYMES

## Abstract

Methods of weight management for a subject are provided. Generally the methods comprising: administering an effective amount to the small intestine and/or large intestine of the subject of at least one agent that increases oxygen tension and/or redox potential and/or pH in the colon of the subject to thereby manage the weight of the subject. Also provided are compositions comprising at least one agent that increases oxygen tension and/or redox potential and/or pH, wherein the composition is formulated for delivery of an effective amount of the at least one agent to the small intestine and/or large intestine of a subject following oral ad ministration of the composition to the subject.

## Claims

### Claim 1

A method of weight management for a human subject in need thereof, the method comprising steps of:
orally administering to a subject who is overweight or obese an enterically-coated oxygen-releasing composition comprising sodium percarbonate,
wherein the enterically-coated oxygen-releasing composition is characterized in that it achieves release of oxygen when assayed in PBS buffer at pH 7.4 after immersion at pH 1.2 for 2 hours.

### Claim 2 (depends on 1)

The method of claim 1, wherein the weight management comprises at least one of weight loss, maintenance of weight loss, avoiding weight gain, body mass index (BMI) reduction, maintenance of BMI reduction, and avoiding BMI gain.

### Claim 3 (depends on 1)

The method of claim 1, wherein the weight management comprises reducing the weight of the subject by at least 5%.

### Claim 4 (depends on 3)

The method of claim 3, wherein the weight management comprises reducing the weight of the subject by at least 10%.

### Claim 5 (depends on 1)

The method of claim 1, wherein the composition is further characterized in that, when contacted with a sample containing both anaerobic and aerobic bacteria, an increase in the relative abundance of aerobic bacteria is achieved.

### Claim 6 (depends on 5)

The method of claim 5, wherein the relative abundance of bacteria in the phylum Proteobacteria is increased.

### Claim 7 (depends on 1)

The method of claim 1, wherein the enteric coating dissolves at a pH above 6.0.

### Claim 8 (depends on 1)

The method of claim 1, wherein the enteric coating dissolves at a pH above 7.0.

### Claim 9 (depends on 1)

The method of claim 1, wherein the composition is formulated for sustained release.

### Claim 10 (depends on 1)

The method of claim 1, wherein the release of oxygen is measured by a dissolved oxygen meter.

### Claim 11

A method of weight management for a human subject in need thereof, the method comprising:
orally administering to a subject who is overweight or obese an oxygen-releasing composition formulated for enteric delivery of its active to the small intestine and/or large intestine of the subject, wherein the active is or comprises sodium percarbonate.

### Claim 12 (depends on 11)

The method of claim 11, wherein the weight management comprises at least one of weight loss, maintenance of weight loss, avoiding weight gain, body mass index (BMI) reduction, maintenance of BMI reduction, and avoiding BMI gain.

### Claim 13 (depends on 11)

The method of claim 11, wherein the weight management comprises reducing the weight of the subject by at least 5%.

### Claim 14 (depends on 13)

The method of claim 13, wherein the weight management comprises reducing the weight of the subject by at least 10%.

### Claim 15 (depends on 11)

The method of claim 11, wherein the relative abundance of at least one of aerobic bacteria and facultative anaerobic bacteria in the microbiota of the colon of the subject is increased by at least 100%.

### Claim 16 (depends on 15)

The method of claim 15, wherein the relative abundance of bacteria in the phylum Proteobacteria is increased in the microbiota of the colon of the subject by at least 100%.

### Claim 17 (depends on 11)

The method of claim 11, wherein the active is administered at a dose of 5 mg to 100 mg of hydrogen peroxide equivalent.

### Claim 18 (depends on 11)

The method of claim 11, wherein the active is administered at a dose of 20 mg to 40 mg of hydrogen peroxide equivalent.

### Claim 19 (depends on 11)

The method of claim 11, wherein the composition is administered as an oral dosage form comprising the active and an enteric coating encasing the active.

### Claim 20 (depends on 19)

The method of claim 19, wherein the enteric coating dissolves at a pH above 6.0.

### Claim 21 (depends on 19)

The method of claim 19, wherein the enteric coating dissolves at a pH above 7.0.

### Claim 22 (depends on 19)

The method of claim 19, wherein the oral dosage form is formulated for sustained release.

### Claim 23

In a method of managing weight by inducing weight loss in an overweight or obese subject who is a candidate for bariatric surgery, the improvement that comprises:
instead of performing bariatric surgery on the subject, orally administering to the subject an oxygen-releasing composition formulated for enteric delivery of its active in the small and/or large intestine, wherein the active is or comprises sodium percarbonate.

### Claim 24

In a method of managing weight by inducing weight loss in an overweight or obese subject who is a candidate for bariatric surgery, the improvement that comprises:
instead of performing bariatric surgery on the subject, orally administering to the subject a composition that is an enteric oxygen delivery composition comprising sodium percarbonate and characterized in that it releases oxygen when assayed in PBS buffer at pH 7.4 after immersion at pH 1.2 for 2 hours.

### Claim 25

In a method of managing weight by inducing weight loss in an overweight or obese subject who is a candidate for bariatric surgery, the improvement that comprises:
instead of performing bariatric surgery on the subject, orally administering an enterically coated oral dosage form of an oxygen-releasing composition comprising sodium percarbonate.

### Claim 26

A method comprising a step of:
orally administering to a subject who is overweight or obese an enterically coated oxygen-releasing composition comprising sodium percarbonate.

### Claim 27

A method comprising a step of:
administering to an overweight or obese subject a composition comprising sodium percarbonate that is an enteric oxygen delivery composition in that it achieves delivery preferentially to the small and/or large intestine.
