# US 2021/0330682 A1 · Compositions and methods for delivering therapeutic agents into the colon

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2021/0330682 A1
- Document ID: US20210330682A1
- Status: Published application
- Kind: A1
- Application number: 17/332,506
- Filed: 2021-05-27
- Published: 2021-10-28
- Earliest claimed: 2015-05-04
- Assignees: The Board of Trustees of the Leland Stanford Junior University
- Applicants: The Board of Trustees of the Leland Stanford Junior University
- Inventors: Sidhartha Ranjit SINHA; Jayakumar RAJADAS; Aida HABTEZION; Ravinder D. PAMNANI
- Web page: https://patentgrep.com/patent/US20210330682A1

## CPC

- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 9/0031: {Rectum, anus}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)}
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 31/60: Salicylic acid; Derivatives thereof
- A61K 31/606: having amino groups
- A61K 31/655: Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- A61K 47/30: Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- C08L 71/02: Polyalkylene oxides
- A61K 9/1272: comprising non-phosphatidyl surfactants as bilayer-forming substances, e.g. cationic lipids or non-phosphatidyl liposomes coated or grafted with polymers (lipids as modifying agents {A61K47/543})
- C08G 2650/58: Ethylene oxide or propylene oxide copolymers, e.g. pluronics
- 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
- C08L: COMPOSITIONS OF MACROMOLECULAR COMPOUNDS (compositions based on polymerisable monomers C08F, C08G; artificial filaments or fibres D01F; textile treating compositions D06)
- C08G: MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS

## Abstract

Enema compositions containing corticosteroids or salicylic acid derivatives are disclosed. The compositions are liquid at room temperature but turn to gels at body temperature. They are useful for treating inflammatory bowel disease.

## Claims

### Claim at position 1

1-18. (canceled)

### Claim 19

A method of making an enema composition, the method comprising:
combining an active agent in a dry, non-aqueous form with water, a thermo-active polymer, and one or more lipids to produce a lipidic suspension into which the active agent is dispersed, thereby creating an enema composition.

### Claim 20 (depends on 19)

The method of claim 19, wherein the combining step comprises:
combining the dry, non-aqueous form of the active agent, water, and the one or more lipids to create a mixture; and
adding the thermo-active polymer to the mixture to create the lipidic suspension.

### Claim 21 (depends on 20)

The method of claim 20, wherein the thermo-active polymer is added to the mixture as an aqueous solution.

### Claim 22 (depends on 20)

The method of claim 20, wherein the thermo-active polymer is added to the mixture in a non-aqueous form.

### Claim 23 (depends on 19)

The method of claim 19, wherein the combining step comprises:
combining the dry, non-aqueous form of the active agent, the thermo-active polymer, and the one or more lipids to create a mixture; and
adding water to the mixture to create the lipidic suspension.

### Claim 24 (depends on 19)

The method of claim 19, wherein the thermo-active polymer is a non-ionic block copolymer consisting of polyethylene glycol and polypropylene glycol blocks.

### Claim 25 (depends on 24)

The method of claim 24, wherein the non-ionic block copolymer is a triblock copolymer having a polyoxypropylene molecular mass of about 4,000 g/mol and about 70% polyoxyethylene content.

### Claim 26 (depends on 24)

The method of claim 24, wherein the non-ionic block copolymer is a triblock copolymer having a polyoxypropylene molecular mass of about 1,800 g/mol and about 80% polyoxyethylene content.

### Claim 27 (depends on 24)

The method of claim 24, wherein the enema composition comprises the thermo-active polymer at from 100 g/L to 400 g/L.

### Claim 28 (depends on 19)

The method of claim 19, wherein the active agent is a salicylic acid derivative.

### Claim 29 (depends on 28)

The method of claim 28, wherein the salicylic acid derivative is selected from the group consisting of mesalazine, sulfasalazine, olsalazine, and balsalazide.

### Claim 30 (depends on 29)

The method of claim 29, wherein the salicylic acid derivative is mesalazine.

### Claim 31 (depends on 1280)

The method of claim 1280, wherein the enema composition comprises the salicylic acid derivative at from 50 g/L to 100 g/L.

### Claim 32 (depends on 19)

The method of claim 19, wherein the active agent is a corticosteroid.

### Claim 33 (depends on 32)

The method of claim 32, wherein the corticosteroid is selected from the group consisting of budesonide, dexamethasone, hydrocortisone, methylprednisolone, prednisolone, and prednisone.

### Claim 34 (depends on 33)

The method of claim 33, wherein the corticosteroid is budesonide.

### Claim 35 (depends on 32)

The method of claim 32, wherein the enema composition comprises the corticosteroid at from 0.05 g/L to 5 g/L.

### Claim 36 (depends on 19)

The method of claim 19, wherein the one or more lipids comprises at least one of dipalmitoylphosphatidylcholine (DPPC) and 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC).

### Claim 37 (depends on 36)

The method of claim 36, wherein the enema composition comprises the one or more lipids at from 4 g/L to 40 g/L.

### Claim 38 (depends on 19)

The method of claim 19, wherein the enema composition exhibits a gel transition temperature between 32° C. and 38° C.