# US 10,945,992 B1 · Dosage forms of rofecoxib and related methods

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- Number: US 10,945,992 B1
- Document ID: US10945992B1
- Status: Granted
- Kind: B1
- Application number: 16/867,514
- Filed: 2020-05-05
- Granted: 2021-03-16
- Earliest claimed: 2019-11-13
- Assignees: Tremeau Pharmaceuticals, Inc.
- Applicants: Tremeau Pharmaceuticals, Inc.
- Inventors: Bradford C. Sippy; Raymond D. Skwierczynski; Travis E. Helm
- Web page: https://patentgrep.com/patent/US10945992B1

## CPC

- A61K 31/365: Lactones
- A61K 9/16: Agglomerates; Granulates; Microbeadlets {; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction (A61K9/20 takes precedence if the final form is a tablet; microspheres with drug-free outer coating, microcapsules A61K9/50; mixture of different granules, microcapsules, (coated) microparticles A61K9/5084; nanoparticles A61K9/51)}
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- 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

The subject matter disclosed herein relates to novel doses and dosage forms of rofecoxib having a therapeutic benefit.

## Claims

### Claim 1

A method for treating pain, fever, or inflammation in a human subject, the method comprising orally administering to the subject once daily a solid dosage formulation comprising 17.5 mg of rofecoxib, wherein the formulation achieves a mean Cmax plasma concentration of more than 180 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 2 (depends on 1)

The method of claim 1, wherein the method comprises treating pain, fever, or inflammation associated with one or more of the following diseases or conditions: migraine associated with von Willebrand deficiency; rheumatoid arthritis (RA); pauciarticular or polyarticular course Juvenile Rheumatoid Arthritis; acute pain; primary dysmenorrhea; migraine attacks with or without aura; chronic lower back pain; psoriatic arthritis; fibromyalgia; and hemophilic arthropathy.

### Claim 3 (depends on 1)

The method of claim 1, wherein the formulation achieves a mean Cmax plasma concentration of more than 190 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 4 (depends on 1)

The method of claim 1, wherein the formulation achieves a mean Cmax plasma concentration of more than 200 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 5 (depends on 4)

The method of claim 4, wherein the formulation achieves a mean Cmax plasma concentration of about 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 6 (depends on 1)

The method of claim 1, wherein the formulation achieves a mean Cmax plasma concentration within 80-125% of 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 7 (depends on 1)

The method of claim 1, wherein the formulation achieves a mean plasma AUC0-∞ of more than 3000 h*ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 8 (depends on 1)

The method of claim 1, wherein the formulation achieves a higher mean plasma Cmax and a higher mean plasma AUC0-∞ in a population of healthy female adults less than 65 years of age compared to a population of healthy male adults less than 65 years of age following oral administration of a single dose of the formulation.

### Claim 9 (depends on 1)

The method of claim 1, wherein the formulation achieves a higher mean plasma AUC0-∞ in Caucasian adults less than 65 years of age compared to healthy African American adults less than 65 years of age following oral administration of a single dose of the formulation.

### Claim 10 (depends on 1)

The method of claim 1, wherein the formulation achieves an arithmetic mean plasma concentration of at least 2.0 ng/ml at 15 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 11 (depends on 1)

The method of claim 1, wherein the formulation achieves an arithmetic mean plasma concentration of at least 79 ng/ml at 45 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 12 (depends on 2)

The method of claim 2, wherein the method comprises treating pain, fever, or inflammation associated with one or more of the following diseases or conditions: chronic lower back pain, psoriatic arthritis, fibromyalgia, hemophilic arthropathy, and migraine associated with von Willebrand deficiency.

### Claim 13 (depends on 2)

The method of claim 2, wherein the method comprises treating pain, fever, or inflammation that is associated with hemophilic arthropathy.

### Claim 14 (depends on 1)

The method of claim 1, wherein the solid dosage formulation further comprises a disintegrant.

### Claim 15

A method for treating pain, fever, or inflammation in a human subject, the method comprising orally administering to the subject once daily a solid dosage formulation comprising 17.5 mg of rofecoxib, wherein the formulation achieves a mean plasma AUC0-∞ of more than 3000 h*ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 16 (depends on 15)

The method of claim 15, wherein the method comprises treating pain, fever, or inflammation associated with one or more of the following diseases or conditions: migraine associated with von Willebrand deficiency; rheumatoid arthritis (RA); pauciarticular or polyarticular course Juvenile Rheumatoid Arthritis; acute pain; primary dysmenorrhea; migraine attacks with or without aura; chronic lower back pain; psoriatic arthritis; fibromyalgia; and hemophilic arthropathy.

### Claim 17 (depends on 15)

The method of claim 15, wherein the formulation achieves a mean Cmax plasma concentration of more than 167 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 18 (depends on 17)

The method of claim 17, wherein the formulation achieves a mean Cmax plasma concentration of about 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 19 (depends on 15)

The method of claim 15, wherein the formulation achieves a mean Cmax plasma concentration within 80-125% of 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 20 (depends on 15)

The method of claim 15, wherein the formulation achieves a higher mean plasma Cmax and a higher mean plasma AUC0-∞ in a population of healthy female adults less than 65 years of age compared to a population of healthy male adults less than 65 years of age following oral administration of a single dose of the formulation.

### Claim 21 (depends on 15)

The method of claim 15, wherein the formulation achieves a higher mean plasma AUC0-∞ in Caucasian adults less than 65 years of age compared to healthy African American adults less than 65 years of age following oral administration of a single dose of the formulation.

### Claim 22 (depends on 15)

The method of claim 15, wherein the formulation achieves an arithmetic mean plasma concentration of at least 79 ng/ml at 45 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 23 (depends on 16)

The method of claim 16, wherein the method comprises treating pain, fever, or inflammation that is associated with one or more of the following diseases or conditions: chronic lower back pain, psoriatic arthritis, fibromyalgia, hemophilic arthropathy, and migraine associated with von Willebrand deficiency.

### Claim 24 (depends on 16)

The method of claim 16, wherein the method comprises treating pain, fever, or inflammation that is associated with hemophilic arthropathy.

### Claim 25 (depends on 15)

The method of claim 15, wherein the solid dosage formulation further comprises a disintegrant.

### Claim 26

A method for treating pain, fever, or inflammation in a human subject, the method comprising orally administering to the subject once daily a solid dosage formulation comprising 17.5 mg of rofecoxib, wherein the formulation achieves an arithmetic mean plasma concentration of at least 2.0 ng/ml at 15 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 27 (depends on 26)

The method of claim 26, wherein the formulation achieves an arithmetic mean plasma concentration of at least 79 ng/ml at 45 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age.

### Claim 28 (depends on 26)

The method of claim 26, wherein the solid dosage formulation further comprises a disintegrant.