# US 12,109,270 B2 · Rifaximin complexes

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- Number: US 12,109,270 B2
- Document ID: US12109270B2
- Status: Granted
- Kind: B2
- Application number: 17/862,491
- Filed: 2022-07-12
- Published: 2023-06-15
- Granted: 2024-10-08
- Earliest claimed: 2008-12-10
- Assignees: Cipla Limited
- Applicants: Cipla Limited
- Inventors: Maruti Ganpati Ghagare; Sunilkumar Parasnath Saroj; Dharmaraj Ramachandra Rao; Rajendra Narayanrao Kankan
- Web page: https://patentgrep.com/patent/US12109270B2

## CPC

- A61K 47/40: Cyclodextrins; Derivatives thereof
- A61K 9/2095: {Tabletting processes}
- A61K 31/4184: condensed with carbocyclic rings, e.g. benzimidazoles
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- 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 47/58: obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
- A61K 47/6951: {using cyclodextrin (cyclodextrins used as simple excipients A61K47/40)}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/12: Antidiarrhoeals
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 9/12: Antihypertensives
- A61P 13/08: of the prostate
- A61P 31/04: Antibacterial agents
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex and therapeutic uses of the complex.

## Claims

### Claim 1

A method of treating bowel disorders, the method comprising:
administering to a patient a therapeutically effective amount of a complex comprising rifaximin and a complexing agent, wherein the complex is in an amorphous form and exhibits enhanced solubility compared to a physical mixture of rifaximin and the complexing agent.

### Claim 2 (depends on 1)

The method of claim 1, wherein the complex is a component of a tablet, a pellet, or a capsule.

### Claim 3 (depends on 1)

The method of claim 1, wherein the bowel disorder is travelers' diarrhea.

### Claim 4 (depends on 1)

The method of claim 1, wherein the bowel disorder is a bowel disease.

### Claim 5 (depends on 1)

The method of claim 1, wherein the bowel disorder is irritable bowel syndrome, Crohn's disease, chronic pancreatitis, pancreatic insufficiency and/or colitis.

### Claim 6 (depends on 1)

The method of claim 1, wherein the bowel disorder is microbe associated diarrhea.

### Claim 7 (depends on 1)

The method according to claim 1, wherein the ratio of rifaximin to complexing agent ranges from 20:1 to 1:20 w/w.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the ratio of rifaximin to complexing agent ranges from 10:1 w/w to 1:2 w/w.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the rifaximin complex is administered with one or more pharmaceutically acceptable excipients.

### Claim 10

A method of treating bowel disorders, the method comprising:
administering to a patient a therapeutically effective amount of a complex comprising rifaximin and a complexing agent,
wherein the complex is in an amorphous form and exhibits enhanced solubility compared to a physical mixture of rifaximin and the complexing agent, the complex is a component of a tablet, and the rifaximin complex is administered with one or more pharmaceutically acceptable excipients.

### Claim 11

A method of treating bowel disorders, the method comprising:
administering to a patient a therapeutically effective amount of a complex comprising rifaximin and a complexing agent,
wherein the complex is in an amorphous form and exhibits enhanced solubility compared to a physical mixture of rifaximin and the complexing agent, the complex is a component of a tablet or a capsule, the bowel disorder is a bowel disease, and the rifaximin complex is administered with one or more pharmaceutically acceptable excipients.

### Claim 12

A method of treating bowel disorders, the method comprising:
administering to a patient a therapeutically effective amount of a complex comprising rifaximin and a complexing agent,
wherein the complex is in an amorphous form and exhibits enhanced solubility compared to a physical mixture of rifaximin and the complexing agent, the complex is a component of a tablet or a capsule, the bowel disorder is microbe associated diarrhea, and the rifaximin complex is administered with one or more pharmaceutically acceptable excipients.
