# US 11,077,124 B2 · Pharmaceutical compositions

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- Number: US 11,077,124 B2
- Document ID: US11077124B2
- Status: Granted
- Kind: B2
- Application number: 15/645,513
- Filed: 2017-07-10
- Published: 2017-11-23
- Granted: 2021-08-03
- Earliest claimed: 2010-07-16
- Assignees: Cipla Limited
- Applicants: CIPLA Limited
- Inventors: Geena Malhotra; Shrinivas Madhukar Purandare; Amar Lulla
- Web page: https://patentgrep.com/patent/US11077124B2

## CPC

- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61K 9/008: {comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]}
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/138: Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine (atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377)
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46)
- A61K 31/46: 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
- A61K 31/4704: 2-Quinolinones, e.g. carbostyril
- A61K 31/4709: Non-condensed quinolines and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 11/08: Bronchodilators
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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

A pharmaceutical composition for inhalation comprising R (+) budesonide and one or more bronchodilators, and, optionally, one or more pharmaceutically acceptable excipients is described.

## Claims

### Claim 1

A pharmaceutical composition for use in treatment of at least one of asthma and COPD comprising a fixed dose combination consisting of R-(+)-budesonide and arformoterol, and, optionally, one or more pharmaceutically acceptable excipients,
wherein R (+) budesonide is present in an amount ranging from 80-640 mcg and arformoterol is present in an amount ranging from 2.4-20.4 mcg; and,
wherein said fixed dose combination of the R-(+)-budesonide and arformoterol is formulated for administration once per day.

### Claim 2 (depends on 1)

A pharmaceutical composition according to claim 1, formulated as an inhalation composition.

### Claim 3 (depends on 1)

A pharmaceutical composition according to claim 1, formulated for use in a metered dose inhaler.

### Claim 4 (depends on 3)

A pharmaceutical composition according to claim 3, comprising a propellant.

### Claim 5 (depends on 1)

A pharmaceutical composition according claim 1, comprising an excipient selected from a co-solvent, an antioxidant, a surfactant, a bulking agent and a lubricant.

### Claim 6 (depends on 1)

A pharmaceutical composition according to claim 1, formulated for use as a dry powder inhalation formulation.

### Claim 7 (depends on 1)

A pharmaceutical composition according to claim 1, comprising at least one finely divided pharmaceutically acceptable carrier suitable for use in dry powder inhalation formulations.

### Claim 8 (depends on 7)

A combination composition according to claim 7, wherein said carrier includes a saccharide and/or a sugar alcohol.

### Claim 9 (depends on 1)

A combination composition according to claim 1, formulated for use as an inhalation solution.

### Claim 10 (depends on 9)

A combination composition according to claim 9, comprising an excipient selected from a wetting agent, osmotic agent, a pH regulator, a buffering agent and a complexing agent, provided in a pharmaceutically acceptable vehicle.

### Claim 11 (depends on 1)

A pharmaceutical composition according to claim 1, formulated for inhalation, for use as a nasal spray, for use as nasal drops, for use as an insufflation powder, or for use as a spray patch.

### Claim 12

A pharmaceutical composition for use in treatment of at least one of asthma and COPD comprising a fixed dose combination consisting of R-(+)-budesonide and arformoterol, and, optionally, one or more pharmaceutically acceptable excipients,
formulated in a metered multi-dose container, wherein the metered multi-dose container contains (quantity/container):
R (+) Budesonide 16 mg, and
Arformoterol tartarate 0.48 mg;
wherein said fixed dose combination of the R-(+)-budesonide and arformoterol is formulated for administration once per day.

### Claim 13 (depends on 12)

A pharmaceutical composition according to claim 12, wherein the metered multi-dose container further contains one or more propellants selected from:
1,1,1,2-tetrafluoroethane,
1,1,1,2,3,3,3,-heptafluoropropane,
difluoromethane,
1,1,1-trifluoroethane,
1,1,2,2-tetrafluoroethane, and
1,1-difluoroethane.

### Claim 14 (depends on 12)

A pharmaceutical composition according to claim 12, wherein the metered multi-dose container contains (quantity/container):
R (+) Budesonide 16 mg,
Arformoterol tartarate 0.48 mg, and
1,1,1,2-tetrafluoroethane (HFA-134(a)) propellant 9.6 g.

### Claim 15 (depends on 12)

A pharmaceutical composition according to claim 12, wherein the metered multi-dose container contains (quantity/container):
R (+) Budesonide 16 mg,
Arformoterol tartarate 0.48 mg,
2% Ethanol 0.22 g,
0.22% Lecithin 0.0003 mg, and
1,1,1,2,3,3,3,-heptafluoropropane (HFA-227) propellant 11.0 g.

### Claim 16 (depends on 12)

A pharmaceutical composition according to claim 12, wherein the metered multi-dose container contains (quantity/container):
R (+) Budesonide 16 mg,
Arformoterol tartarate 0.48 mg, and
1,1,1,2,3,3,3,-heptafluoropropane (HFA-227) propellant 11.2 g.

### Claim 17 (depends on 12)

A pharmaceutical composition according to claim 12, wherein the metered multi-dose container contains (quantity/container):
R (+) Budesonide 16 mg,
Arformoterol tartarate 0.48 mg,
0.3% PEG 1000 33.6 mg,
0.001% polyvinylpyrrolidone (PVP K25) 0.11 mg, and
1,1,1,2,3,3,3,-heptafluoropropane (HFA-227) propellant 11.2 g.

### Claim 18 (depends on 12)

A pharmaceutical composition according to claim 12, comprising at least one finely divided pharmaceutically acceptable carrier suitable for use in dry powder inhalation formulations.

### Claim 19 (depends on 18)

A combination composition according to claim 18, wherein said carrier includes a saccharide and/or a sugar alcohol.

### Claim 20 (depends on 12)

A combination composition according to claim 12, formulated for use as an inhalation solution.

### Claim 21 (depends on 20)

A combination composition according to claim 20, comprising an excipient selected from a wetting agent, osmotic agent, a pH regulator, a buffering agent and a complexing agent, provided in a pharmaceutically acceptable vehicle.

### Claim 22 (depends on 12)

A pharmaceutical composition according to claim 12, formulated for inhalation, for use as a nasal spray, for use as nasal drops, for use as an insufflation powder, or for use as a spray patch.