# US 11,026,882 B2 · Methods and compositions for treating migraine and conditions associated with pain

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- Number: US 11,026,882 B2
- Document ID: US11026882B2
- Status: Granted
- Kind: B2
- Application number: 16/234,069
- Filed: 2018-12-27
- Published: 2019-07-18
- Granted: 2021-06-08
- Earliest claimed: 2014-12-01
- Assignees: Achelios Therapeutics, Inc.
- Applicants: Achelios Therapeutics, Inc.
- Inventors: Crist J. Frangakis; William Bauer; Wolfgang Liedtke
- Web page: https://patentgrep.com/patent/US11026882B2

## CPC

- 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 31/14: Quaternary ammonium compounds, e.g. edrophonium, choline (betaines A61K31/205)
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
- A61K 31/405: Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
- A61K 31/407: condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
- A61K 31/415: 1,2-Diazoles
- A61K 31/5415: ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
- A61K 31/616: by carboxylic acids, e.g. acetylsalicylic acid
- A61K 31/635: having a heterocyclic ring, e.g. sulfadiazine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61P 25/06: Antimigraine agents
- 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 pharmaceutical compositions of a non-steroidal anti-inflammatory drug (NSAIDs) such as, aspirin, diclofenac, ibuprofen, ketoprofen, or naproxen, or any pharmaceutically acceptable salts, solvates, or prodrugs thereof, and the medical use of these compositions. The compositions, which can be formulated for topical administration, can provide extended release of the NSAIDs. The compositions of the invention are useful, for example, in the prophylactic treatment or treatment and/or reduction of pain, in the prophylactic treatment or treatment of headaches such as migraine headaches and symptoms of migraine headaches, and in the treatment of temporomandibular disorders (TMD).

## Claims

### Claim 1

A method of treating pain or inflammation associated with a temporomandibular disorder (TMD) in a subject in need thereof, said method comprising topically administering to said subject a sustained release composition comprising from about 0.5% (w/w) to about 5% (w/w) of a therapeutic agent and a dermatologically acceptable excipient, wherein said composition is in an amount effective to treat said temporomandibular disorder (TMD) in said subject; wherein administration of said composition to said subject results in a peak plasma concentration of said therapeutic agent at three hours that is at most about 450 ng/mL; wherein said therapeutic agent is ketoprofen; and wherein said composition comprises from about 20 mg to about 200 mg of ketoprofen in unit dosage form.

### Claim 2 (depends on 1)

The method of claim 1, wherein said peak plasma concentration of said therapeutic agent when administered topically is lower than the peak plasma concentration of said therapeutic agent when administered orally.

### Claim 3 (depends on 1)

The method of claim 1, wherein administration of said composition to said subject provides for gradual release of said therapeutic agent over 2-24 hours.

### Claim 4 (depends on 3)

The method of claim 3, wherein administration of said composition results in a plasma concentration of said therapeutic agent that is maintained between about 50 ng/mL and about 150 ng/mL for up to 24 hours.

### Claim 5 (depends on 1)

The method of claim 1, wherein the half-life of said therapeutic agent is from about 7 to about 13 hours.

### Claim 6 (depends on 1)

The method of claim 1, further comprising monitoring whether the subject experiences amelioration of the pain or inflammation associated with TMD.

### Claim 7 (depends on 1)

The method of claim 1, wherein said composition comprises a total maximum dosage of about 135 mg of ketoprofen.

### Claim 8 (depends on 1)

The method of claim 1, wherein said composition is formulated as a gel, cream, lotion, ointment, foam, powder, solution, spray, emulsion, or suspension for topical administration.

### Claim 9 (depends on 8)

The method of claim 8, wherein said composition if formulated as a gel for topical administration.

### Claim 10 (depends on 1)

The method of claim 1, wherein said composition is administered one or more times a day.

### Claim 11 (depends on 1)

The method of claim 1, wherein said composition is administered for one day or at least two to twenty days.

### Claim 12 (depends on 1)

The method of claim 1, wherein said composition is administered for more than twenty days.

### Claim 13 (depends on 1)

The method of claim 1, wherein said composition is administered with a second agent.

### Claim 14 (depends on 13)

The method of claim 13, wherein said second agent is selected from the group consisting of: a corticosteroid, acetaminophen, an opioid, a muscle relaxant, an anti-anxiety drug, an anti-depressant, an anti-convulsant drug, an antipsychotic, an antiepileptic drug, and a selective serotonin reuptake inhibitor (SSRI).