# US 11,110,077 B2 · Apremilast pharmaceutical compositions

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

- Number: US 11,110,077 B2
- Document ID: US11110077B2
- Status: Granted
- Kind: B2
- Application number: 16/088,801
- Filed: 2016-09-30
- Published: 2019-02-14
- Granted: 2021-09-07
- Earliest claimed: 2016-03-30
- Assignees: Sarudbhava Formulations Private Limited
- Applicants: Sarudbhava Formulations Private Limited
- Inventors: Venkata Nookaraju Sreedharala
- Web page: https://patentgrep.com/patent/US11110077B2

## CPC

- A61K 31/4035: Isoindoles, e.g. phthalimide
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
- A61P 17/06: Antipsoriatics
- 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

## Abstract

The present invention relates to topical pharmaceutical compositions of apremilast used for the treatment of psoriasis and/or psoriatic arthritis. It further relates to processes of preparation of the compositions and the method of use for these compositions.

## Claims

### Claim 1

A topical pharmaceutical composition of apremilast, comprising:
a. 1-5% w/w of apremilast or pharmaceutically acceptable salt thereof;
b. a first pharmaceutically acceptable carrier at a concentration range of 5-30% w/w; and
c. a pharmaceutically acceptable excipient;
wherein the first pharmaceutically acceptable carrier is selected from the group consisting of dimethyl sulfoxide, glycerol, propylene glycol, petrolatum, water, and a mixture thereof,
wherein the pH of the said composition is ranging from pH 3 to 8, and
wherein the said topical composition has the ratio of apremilast to carrier in the range of 1:100 to 100:1.

### Claim 2 (depends on 1)

A topical pharmaceutical composition of claim 1, wherein the topical pharmaceutical composition is a cream.

### Claim 3 (depends on 1)

A topical pharmaceutical composition of claim 1, wherein the topical pharmaceutical composition is an ointment.

### Claim 4 (depends on 1)

A topical pharmaceutical composition of claim 1, wherein the topical pharmaceutical composition is a spray.

### Claim 5 (depends on 1)

The topical pharmaceutical composition of claim 1, wherein the pharmaceutically acceptable excipient is selected from the group comprising of skin penetration enhancer, pharmaceutical surfactants, solubility enhancers, oil phase components, aqueous phase components, emulsifiers, anti-oxidants, vitamins, lubricants, preservatives, stabilizers, buffers and mixture thereof.

### Claim 6 (depends on 1)

The topical pharmaceutical composition of claim 1, wherein the pH of the composition is maintained in the range from pH 3 to 8 using pH adjusting agents selected from hydrochloric acid, phosphoric acid, lactic acid, diethanolamine, triethanolamine, sodium hydroxide, monobasic sodium phosphate, dibasic sodium phosphate, or a mixture thereof.

### Claim 7 (depends on 1)

The topical pharmaceutical composition of claim 1, wherein the pharmaceutically acceptable excipient is a surfactant or emulsifier selected from polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, sorbitan ester, sorbitan oleate, sorbitan stearate, polyoxyethylene stearate, sodium lauryl sulphate, stearyl alcohol, poly alkylene glycol ether or a mixture thereof.

### Claim 8 (depends on 1)

The topical pharmaceutical composition of claim 1, wherein the carrier in the composition is selected from penetration enhancer, diluent, solubility enhancer, vehicle and a pharmaceutical adjuvant.

### Claim 9 (depends on 1)

The topical pharmaceutical composition of claim 1, wherein the said composition is for alleviating or slowing the symptoms of psoriasis within 5 days of administration to a patient that has manifested clinical disease.

### Claim 10 (depends on 1)

The topical pharmaceutical composition of claim 1, wherein the said composition comprises of apremilast and dimethyl sulfoxide in a ratio of 1:100 to 100:1.

### Claim 11 (depends on 1)

The topical pharmaceutical composition of claim 1, wherein the said composition comprises of apremilast 1-5% w/w, dimethyl sulfoxide, further comprises 20-90% w/w of a second carrier selected from the group consisting of glycerol, propylene glycol, petrolatum, water, and a mixture thereof; and a pharmaceutical excipient selected from skin penetration enhancer, pharmaceutical surfactants, solubility enhancers, oil phase components, aqueous phase components, emulsifiers, anti-oxidants, vitamins, lubricants, preservatives, stabilizers, buffers or mixture thereof, wherein the ratio of apremilast to dimethyl sulfoxide in the composition is ranging between 1:100 to 100:1.

### Claim 12 (depends on 1)

The topical pharmaceutical composition of claim 1, further comprising a second pharmaceutically acceptable carrier at a concentration range of 20-90%, wherein the second pharmaceutically acceptable carrier is selected from the group consisting of dimethyl sulfoxide, glycerol, propylene glycol, petrolatum, water, and a mixture thereof.

### Claim 13 (depends on 1)

A topical pharmaceutical composition of claim 1, wherein the topical pharmaceutical composition is a gel.