# US 10,441,530 B2 · Skin penetration enhancing systems for polar drugs

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- Number: US 10,441,530 B2
- Document ID: US10441530B2
- Status: Granted
- Kind: B2
- Application number: 15/697,244
- Filed: 2017-09-06
- Published: 2018-03-22
- Granted: 2019-10-15
- Earliest claimed: 2008-02-15
- Assignees: AmDerma Pharmaceuticals, LLC
- Applicants: AmDerma Pharmaceuticals, LLC
- Inventors: David W. Osborne; Pramod P. Sarpotdar; Arturo J. Angel; Inigo Saenz de Tejada Gorman; Pedro Cuevas Sànchez
- Web page: https://patentgrep.com/patent/US10441530B2

## 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 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)
- A61P 17/00: Drugs for dermatological disorders
- A61K 47/06: Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- 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 47/38: Cellulose; Derivatives thereof
- 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 invention relates to pharmaceutical compositions and related methods for the topical administration of polar drugs. In a particular embodiment, the invention relates to a pharmaceutical composition comprising an active pharmaceutical agent that is a polar drug, such as potassium 2,5-dihydroxybenzenesulfonate, at least one occlusive agent, and at least one stabilizer.

## Claims

### Claim 1

A topical pharmaceutical skin penetration enhancing system, comprising a water-in-oil emulsion that comprises:
(a) about 5 to about 10% by weight of potassium 2,5-dihydroxybenzenesulfonate (potassium dobesilate);
(b) about 50 to about 75% by weight of at least one occlusive agent selected from white petrolatum, mineral oil, and mixtures thereof;
(c) about 0.1 to about 5% by weight of at least one surfactant selected from steareth-2 (Brij 72), steareth-21 (Brij 721), and mixtures thereof;
(d) about 0.1 to about 10% by weight of a stiffening agent selected from stearyl alcohol, cetyl alcohol, and mixtures thereof;
(e) about 0.01 to about 10% by weight of a pH adjuster selected from acetic acid solution, sodium acetate, and mixtures thereof; and
about 0.1 to less than about 22% by weight water.

### Claim 2 (depends on 1)

The system of claim 1, further comprising a preservative, a solvent, and, optionally, an antioxidant.

### Claim 3 (depends on 1)

The system of claim 1, further comprising:
(f) about 0.001 to about 5% by weight of a preservative selected from sodium thiosulfate pentahydrate, benzyl alcohol, parabens, and mixtures thereof.

### Claim 4 (depends on 3)

The system of claim 3, comprising:
(a) about 5 to about 10% by weight potassium 2,5-dihydroxybenzenesulfonate;
(b) about 65 to about 70% by weight white petrolatum, mineral oil, or mixtures thereof;
(c) about 5% by weight steareth-2 (Brij 72), steareth-21 (Brij 721), or mixtures thereof;
(d) about 0.1 to about 2% by weight stearyl alcohol, cetyl alcohol, or mixtures thereof;
(e) about 0.05 to about 1% by weight acetic acid solution, sodium acetate, or mixtures thereof;
(f) about 0.1 to about 1% by weight of benzyl alcohol, sodium thiosulfate pentahydrate, butyl paraben, or mixtures thereof; and
water to 100%.

### Claim 5 (depends on 1)

The system of claim 1, which is administered daily.

### Claim 6 (depends on 1)

The system of claim 1, which is effective for topical treatment of one or more of: rosacea, acne, cancers of the skin, actinic keratosis, dermatitis, and psoriasis.

### Claim 7 (depends on 1)

The system of claim 1, wherein the potassium 2,5-dihydroxybenzenesulfonate is suspended in the emulsion.