# US 2011/0217248 A1 · Topical Composition

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- Number: US 2011/0217248 A1
- Document ID: US20110217248A1
- Status: Published application
- Kind: A1
- Application number: 12/944,014
- Filed: 2010-11-11
- Published: 2011-09-08
- Earliest claimed: 2006-09-06
- Assignees: ISW Group, Inc.
- Inventors: Monique Spann-Wade; Kenton N. Fedde
- Web page: https://patentgrep.com/patent/US20110217248A1

## CPC

- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- 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 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/185: Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids (hydroxamic acids A61K31/16; peroxy acids A61K31/327)
- A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
- A61K 31/21: Esters, e.g. nitroglycerine, selenocyanates
- A61K 31/216: of acids having aromatic rings, e.g. benactizyne, clofibrate
- A61K 31/245: Amino benzoic acid types, e.g. procaine, novocaine (salicylic acid esters A61K31/60)
- A61K 31/404: Indoles, e.g. pindolol
- 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 31/4152: having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
- A61K 31/436: the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/5415: ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/18: Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/06: Antipsoriatics
- A61P 17/08: Antiseborrheics
- A61P 17/16: Emollients or protectives, e.g. against radiation
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Examplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, diproylene glycol, propylene glycol, ethanol, isopropanol, or a derivative therof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn.

## Claims

### Claim 1

A composition comprising an NSAID, a solvent system, and from zero to about 60% alkanol, wherein
(i) the solvent system comprises at least two solvent alcohols;
(ii) one of the at least two solvent alcohols is a polyethylene glycol, a propylene glycol, glycerin, polyether polyol, butylene glycol; or a glycerol derivative;
(iii) the solvent system has at least about a 20% super solvent effect;
(iv) the solvent system is present in an amount sufficient to solubilize the NSAID;
(v) the NSAID is in an amount of about 12% to about 30%; and
(vi) the composition is single phasic.

### Claim 2 (depends on 1)

The composition of claim 1 wherein the other one of at least two solvent alcohols is selected from the group consisting of polyethylene glycols, propylene glycols, glycerin, polyether polyols, butylene glycols; glycerol derivatives, ethanol, and isopropanol.

### Claim 3 (depends on 1)

The composition of claim 1 wherein the NSAID is in an amount of from about 0.25 to about 2 times the value determined by Formula 1.

### Claim 4 (depends on 1)

The composition of claim 1 further comprising at least about 20% water.

### Claim 5 (depends on 1)

The composition of claim 1 wherein the at least two solvent alcohols are polyethylene glycol and propylene glycol in a combined amount of about 40% to about 60% and wherein the composition further comprises water wherein water and the NSAID are in amounts according to W=−0.62D+b where b is 0 to 42.5 [Formula 18] or according to W≦−0.62D+42.5 [Formula 19].

### Claim 6 (depends on 5)

The composition of claim 5, wherein the NSAID has a pKa from about 3.0 to about 6.5 and a log10 P value of about 2 to about 5.5.

### Claim 7 (depends on 1)

The composition of claim 1 wherein, when dermally applied daily, is effective in treating PFB.

### Claim 8 (depends on 1)

The composition of claim 1 wherein the composition further comprises an NSAID prodrug.

### Claim 9 (depends on 1)

The composition of claim 1 further comprising a botanical agent.

### Claim 10 (depends on 1)

The composition of claim 1 wherein one of at least two solvent alcohols is an alkanol and upon storage at room temperature, there is less than 1% NSAID alkanol ester formed.

### Claim 11 (depends on 1)

The composition of claim 1 wherein the alkanol is about 0 to one of about 40%, about 30%, about 20%, or about 10%.

### Claim 12 (depends on 1)

The composition of claim 1 having a viscosity in a range selected from the group of ranges consisting of about 2000 cps to about 200,000 cps, about 50,000 cps to about 200,000 cps, about 50,000 cps to about 100,000 cps, about 2,000 to about 50,000, about 2,000 cps to about 25,000 cps, about 2,000 cps to about 10,000 cps, and about 2,000 cps to about 5,000 cps.

### Claim 13 (depends on 1)

The composition of claim 1 where the Drug is an NSAID prodrug and where the composition further comprises a thickening agent, wherein the NSAID is of the phenylacetic acid-type and the pro-moiety is an amidyl, a thio, or an alkyl in ester linkage to the NSAID.

### Claim 14 (depends on 1)

A method of treating a subject with dermatophytoses, seborrheic dermatitis, or pityriasis capitis comprising applying the composition of claim 1 wherein the composition further comprises an antifungal agent.

### Claim 15 (depends on 1)

A method of treating a subject with a furuncle, Impetigo, a wound, a skin infection, rosacea, or Pseudomonas folliculitis comprising dermally applying the composition of claim 1 wherein the composition further comprises an antibacterial agent

### Claim 16 (depends on 1)

A method of treating a subject in need comprising dermally applying the composition of claim 1 wherein the composition further comprises a corticosteroid and wherein the NSAID is in a corticosteroid-sparing amount.

### Claim 17 (depends on 1)

A method of treating a subject with PFB, dermatitis, sunburn, actinic keratoses, rosacea, vitiligo, a wound, or a skin infection, comprising dermally applying the composition of claim 1 wherein the composition further comprises one or more of a UVA blocker, a UVB blocker, and an antioxidant.

### Claim at position 18 (depends on 1)

18, A method of treating a subject in need comprising dermally applying the composition of claim 1 wherein the composition further comprises an antihistamine.

### Claim 19 (depends on 1)

A method of treating a subject in need comprising dermally applying the composition of claim 1 wherein the composition further comprises a botanical agent.