# US 9,750,756 B2 · Celecoxib compositions

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- Number: US 9,750,756 B2
- Document ID: US9750756B2
- Status: Granted
- Kind: B2
- Application number: 14/493,921
- Filed: 2014-09-23
- Published: 2015-01-08
- Granted: 2017-09-05
- Earliest claimed: 1998-11-30
- Assignees: Pfizer Inc.
- Applicants: Pfizer Inc.
- Inventors: Danchen Gao; Anthony J. Hlinak; Ahmad M. Mazhary; James E. Truelove; Margaret B. Vaughn
- Web page: https://patentgrep.com/patent/US9750756B2

## CPC

- A61K 31/635: having a heterocyclic ring, e.g. sulfadiazine
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2095: {Tabletting processes}
- A61K 9/4858: {Organic compounds}
- A61K 9/4866: {Organic macromolecular compounds}
- A61K 31/415: 1,2-Diazoles
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 7/04: Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
- A61P 7/06: Antianaemics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/04: Antipruritics
- A61P 17/06: Antipsoriatics
- A61P 17/10: Anti-acne agents
- A61P 17/16: Emollients or protectives, e.g. against radiation
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/04: for non-specific disorders of the connective tissue
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 19/10: for osteoporosis
- A61P 21/04: for myasthenia gravis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/06: Antimigraine agents
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 27/14: Decongestants or antiallergics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient}
- 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

Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to about 1000 mg in intimate mixture with one or more pharmaceutically acceptable excipients. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.

## Claims

### Claim 1

A pharmaceutical composition comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to about 1000 mg in intimate mixture with one or more pharmaceutically acceptable excipients, and having a distribution of celecoxib particle sizes such that D90 of the particles is less than 200 um; said composition exhibiting upon oral administration a relative bioavailability not less than about 50% by comparison with an orally delivered solution containing celecoxib at the same dosage rate, wherein said excipients include:
a. one or more pharmaceutically acceptable diluents in a total amount of about 5% to about 99% by weight of the composition;
b. one or more pharmaceutically acceptable disintegrants in a total amount of about 0.2% to about 30% by weight of the composition;
c. one or more pharmaceutically acceptable binding agents in a total amount of about 0.5% to about 25% by weight of the composition;
d. one or more pharmaceutically acceptable wetting agents in a total amount of about 0.25% to about 15% by weight of the composition; and
e. one or more pharmaceutically acceptable lubricants in a total amount of about 0.1% to about 10% by weight of the composition.

### Claim 2 (depends on 1)

The composition of claim 1 wherein the amount of celecoxib in each dose unit is about 50 mg to about 800 mg.

### Claim 3 (depends on 1)

The composition of claim 1 wherein the amount of celecoxib in each dose unit is about 75 mg to about 400 mg.

### Claim 4 (depends on 1)

The composition of claim 1 wherein the amount of celecoxib in each dose unit is about 100 mg to about 200 mg.

### Claim 5 (depends on 1)

A composition of claim 1 that is suitable, by oral administration to a subject of a dose unit once or twice a day, for providing therapeutically or prophylactically effective inhibition of cyclooxygenase-2.

### Claim 6 (depends on 1)

A composition of claim 1 that is suitable, by oral administration to a subject of a dose unit once or twice a day, for treatment or prophylaxis of a cyclooxygenase-2 mediated condition or disorder.

### Claim 7 (depends on 1)

A composition of claim 1 in the form of unit dosage capsules or tablets.