# US 12,109,306 B2 · Hydrocortisone acetate suppository formulation for treatment of disease

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- Number: US 12,109,306 B2
- Document ID: US12109306B2
- Status: Granted
- Kind: B2
- Application number: 18/588,892
- Filed: 2024-02-27
- Published: 2024-06-27
- Granted: 2024-10-08
- Earliest claimed: 2015-03-12
- Assignees: Cristcot LLC
- Applicants: Cristcot LLC
- Inventors: Jennifer J. Davagian; Raj Devarajan
- Web page: https://patentgrep.com/patent/US12109306B2

## CPC

- A61K 9/025: {characterised by shape or structure, e.g. hollow layered, coated}
- A61K 9/0031: {Rectum, anus}
- A61K 9/02: Suppositories; Bougies; Bases therefor; {Ovules}(apparatus for making A61J3/08; devices for introducing into the body A61M31/00)
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 47/02: Inorganic compounds
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
- A61M 31/007: {Injectors for solid bodies, e.g. suppositories}
- A61P 1/06: Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
- A61M 2210/1064: Large intestine
- A61M 2210/1067: Anus
- 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)
- A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)}
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates, in various embodiments, to formulations comprising hydrocortisone and silicon dioxide. In additional embodiments, the invention relates to suppositories comprising hydrocortisone and silicon dioxide. The formulations of the present invention are useful for administration to patients who have gastrointestinal diseases and disorders such as, for example, inflammatory bowel disease.

## Claims

### Claim 1

A method of treating a gastrointestinal disease selected from ulcerative colitis or Crohn's disease, comprising rectally administering to a subject in need thereof a formulation comprising about 0.5% to about 5% by weight hydrocortisone acetate, about 0.1% to about 5% by weight colloidal silicon dioxide, a semi-synthetic glyceride base comprising saturated C8-C18 triglyceride fatty acids, and lecithin, wherein the formulation has a melting temperature in the range of about 37° C. to about 39° C.

### Claim 2 (depends on 1)

The method of claim 1, comprising about 4.5% by weight hydrocortisone acetate and about 0.7% by weight colloidal silicon dioxide.

### Claim 3 (depends on 1)

The method of claim 1, wherein the base comprises at least about 85% C8-C18 triglyceride fatty acids, and further comprises diglycerides and monoglycerides.

### Claim 4 (depends on 1)

The method of claim 1, wherein the formulation releases the hydrocortisone acetate upon exposure to rectal fluid.

### Claim 5 (depends on 1)

The method of claim 1, wherein the formulation is administered in combination with mesalamine.

### Claim 6 (depends on 1)

The method of claim 1, wherein the formulation is administered in combination with a local anesthetic.

### Claim 7 (depends on 6)

The method of claim 6, wherein the local anesthetic is lidocaine.

### Claim 8 (depends on 1)

The method of claim 1, wherein the formulation comprises about 90 mg of hydrocortisone acetate.

### Claim 9 (depends on 1)

The method of claim 1, wherein the formulation comprises about 85 to about 95 mg of hydrocortisone acetate.

### Claim 10 (depends on 1)

The method of claim 1, wherein the formulation comprises 90 mg of hydrocortisone acetate.

### Claim 11 (depends on 1)

The method of claim 1, wherein the formulation comprises 85 to 95 mg of hydrocortisone acetate.

### Claim 12 (depends on 1)

The method of claim 1, wherein the formulation comprises about 94.8% w/w of the semi-synthetic glyceride base.

### Claim 13 (depends on 2)

The method of claim 2, wherein the formulation comprises about 94.8% w/w of the semi-synthetic glyceride base.

### Claim 14 (depends on 13)

The method of claim 13, wherein the formulation comprises 85 to 95 mg of hydrocortisone acetate.

### Claim 15 (depends on 14)

The method of claim 14, wherein the formulation comprises 90 mg of hydrocortisone acetate.

### Claim 16 (depends on 2)

The method of claim 2, wherein the formulation is a suppository with a weight of about 2 grams.

### Claim 17 (depends on 15)

The method of claim 15, wherein the formulation is a suppository with a weight of about 2 grams.