# US 10,765,686 B2 · Stable fixed dose pharmaceutical composition comprising mometasone and olopatadine

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- Number: US 10,765,686 B2
- Document ID: US10765686B2
- Status: Granted
- Kind: B2
- Application number: 15/703,828
- Filed: 2017-09-13
- Published: 2018-01-04
- Granted: 2020-09-08
- Earliest claimed: 2013-09-13
- Assignees: Glenmark Specialty S.A.
- Applicants: Glenmark Specialty S.A.
- Inventors: Ulhas R. Dhuppad; Ashok Katkurwar; Yashwant Gupta; Rajesh Ankam; Chandrakant Dhatrak
- Web page: https://patentgrep.com/patent/US10765686B2

## CPC

- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 9/0043: {Nose}
- A61K 9/10: Dispersions; Emulsions
- A61K 31/335: having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K 47/38: Cellulose; Derivatives thereof
- 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)

## Abstract

The present invention relates to a stable fixed dose aqueous pharmaceutical composition (e.g., contained in a container) for nasal administration to a human, comprising mometasone or its salt, olopatadine or its salt. The composition may further include a hydrocolloid. The invention also relates to a process for preparing the pharmaceutical composition, and the use of the pharmaceutical composition in the treatment of rhinitis in a subject.

## Claims

### Claim 1

A method of delivering a nasal spray comprising:
nasally delivering an aqueous pharmaceutical composition in the form of a single phase suspension, said composition comprising (a) mometasone furoate in particulate form; (b) olopatadine hydrochloride in dissolved form, and (c) a hydrocolloid in an amount sufficient to inhibit phase separation for at least 24 hours when stored at 25±2° C. and 60±5% relative humidity, wherein
the mometasone furoate and olopatadine hydrochloride are the sole active ingredients in the composition, and
the spray provides a droplet size distribution having a D10 of 5-25 μm, a D50 of 20-50 μm, a D90 of 40-120 μm, and a SPAN of not more than 4.

### Claim 2 (depends on 1)

A method of claim 1, wherein the spray provides a droplet size distribution having a D10 of 10-22 μm, D50 of 35-45 μm, and D90 of 75-115 μm, and SPAN is not more than 3.

### Claim 3 (depends on 1)

A method of claim 1, wherein the composition comprises 25 μg mometasone furoate.

### Claim 4 (depends on 1)

A method of claim 1, wherein the composition comprises 665 μg olopatadine hydrochloride.

### Claim 5 (depends on 1)

A method of claim 1, wherein the composition has a pH between 3.3 to 4.1.

### Claim 6

A method of delivering a nasal spray comprising:
nasally delivering an aqueous pharmaceutical composition in the form of a single phase suspension, said composition comprising (a) mometasone furoate in particulate form; (b) olopatadine hydrochloride in dissolved form; and (c) a hydrocolloid in an amount sufficient to inhibit phase separation for at least 24 hours when stored at 25±2° C. and 60±5% relative humidity, wherein
the mometasone furoate and olopatadine hydrochloride are the sole active ingredients in the composition, and
the spray provides a droplet size distribution having a D10 of 5-25 μm, a D50 of 20-50 μm, a D90 of 40-120 μm, and a SPAN of not more than 4,
the composition has a viscosity of 10 to 200 cps, and
the pH of the composition is 3.5 to 3.9.

### Claim 7 (depends on 1)

A method of claim 1, wherein the pH of the composition is 3.5 to 3.7.

### Claim 8 (depends on 1)

A method of claim 1, wherein the mean particle size of the mometasone furoate is from 1 μm to 20 μm.

### Claim 9 (depends on 1)

A method of claim 1, wherein the composition has an osmolality of 250 mOsm/kg to 350 mOsm/kg.

### Claim 10 (depends on 1)

A method of claim 1, wherein the composition has a viscosity of 10 to 200 cps.

### Claim 11 (depends on 1)

A method of claim 1, wherein the composition remains in a single phase after at least 3 months of storage at 25±2° C. and 60%±5% relative humidity.

### Claim 12 (depends on 6)

A method of claim 6, wherein the composition results in a spray pattern having a longest axis of 15-75 mm, a shortest axis of 10-65 mm, and an ellipticity of 1-2.

### Claim 13 (depends on 1)

A method of claim 1, wherein the hydrocolloid comprises carboxymethylcellulose sodium.

### Claim 14 (depends on 1)

A method of claim 1, wherein the composition comprises:
0.025% w/w mometasone furoate monohydrate;
0.665% w/w olopatadine hydrochloride;
0.5% w/w carboxymethyl cellulose sodium;
1.2% w/w of a mixture of microcrystalline cellulose and carboxymethyl cellulose sodium;
0.02% w/w benzalkonium chloride;
0.41% w/w sodium chloride;
0.01% w/w di-sodium edetate;
0.94% w/w dibasic sodium phosphate heptahydrate; and
0.01% w/w polysorbate 80,
wherein the pH is from 3.5 to 3.9.