# US 10,478,452 B2 · Antiviral pharmaceutical composition for topical use

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- Number: US 10,478,452 B2
- Document ID: US10478452B2
- Status: Granted
- Kind: B2
- Application number: 15/573,901
- Filed: 2016-05-13
- Published: 2018-09-06
- Granted: 2019-11-19
- Earliest claimed: 2015-05-15
- Assignees: Quimica Luar SRL
- Applicants: Quimica Luar Srl
- Inventors: Luis Alberto Argañarás; Roxana Valeria Alasino; Dante Miguel Beltramo
- Web page: https://patentgrep.com/patent/US10478452B2

## CPC

- A61K 31/78: of acrylic acid or derivatives thereof
- 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 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/4425: Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
- A61P 31/22: for herpes viruses
- 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 an antiviral pharmaceutical composition for topical use against those viruses with a lipid envelope, comprising, as active ingredients a cationic copolymer containing tertiary amine groups and a cationic surfactant containing quaternary ammonium groups.

## Claims

### Claim 1

An antiviral pharmaceutical composition for topical use against viruses with a lipid envelope, comprising active agents; a facilitating agent; and a cationic polymer, wherein the active ingredients consist of a cationic copolymer containing tertiary amine groups, and a cationic surfactant containing quaternary ammonium groups; wherein the facilitating agent for facilitating passage through skin includes sulfur groups; and wherein the cationic polymer contributes necessary viscosity to allow longer residence time on an applied area and comprises polyquaternium 10.

### Claim 2 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, further comprising an anesthetic for local use.

### Claim 3 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said cationic copolymer comprises an acrylic derivative.

### Claim 4 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said cationic copolymer comprises poly(butylmethacrylate-co-2-dimethylaminoethyl)methacrylate-co-methyl methacrylate) 1:2:1.

### Claim 5 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said cationic copolymer is present at a concentration of between 0.1 and 5% by weight of said antiviral pharmaceutical composition.

### Claim 6 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said cationic copolymer is present at a concentration of between 0.5 and 3% by weight of said antiviral pharmaceutical composition.

### Claim 7 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said cationic copolymer is present at a concentration of between 1 and 2% by weight of said pharmaceutical composition.

### Claim 8 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said cationic surfactant containing quaternary ammonium groups comprises cetylpyridinium chloride.

### Claim 9 (depends on 1)

The antiviral c pharmaceutical composition according to claim 1, wherein said cationic surfactant containing quaternary ammonium groups is present at a concentration of between 0.1 and 2% by weight of said antiviral pharmaceutical composition.

### Claim 10 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said cationic surfactant containing quaternary ammonium groups is present at a concentration of between 0.3 and 0.5% by weight of said antiviral pharmaceutical composition.

### Claim 11 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said facilitating agent comprises dimethylsulfoxide in a concentration of between 2 and 35% by weight of said antiviral pharmaceutical composition.

### Claim 12 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said facilitating agent comprises dimethylsulfoxide in a concentration of between 5 and 20% by weight of said antiviral pharmaceutical composition.

### Claim 13 (depends on 1)

The antiviral pharmaceutical composition according to claim 1, wherein said facilitating agent comprises dimethylsulfoxide in a concentration of between 8 and 15% by weight of said antiviral pharmaceutical composition.

### Claim 14 (depends on 2)

The antiviral pharmaceutical composition according to claim 2, wherein said anesthetic for local use is selected from the group consisting of lidocaine, xylocaine, bupivacaine, tetracaine, mepivacaine, prilocaine, butacaine, procaine, ropivacaine and mixtures thereof, and is present at a concentration of between 1 and 15% by weight of said antiviral pharmaceutical composition.

### Claim 15 (depends on 2)

The antiviral pharmaceutical composition according to claim 2, wherein said anesthetic for local use is selected from the group consisting of lidocaine, xylocaine, bupivacaine, tetracaine, mepivacaine, prilocaine, butacaine, procaine, ropivacaine and mixtures thereof, and is present at a concentration of between 2 and 10% by weight of said antiviral pharmaceutical composition.

### Claim 16 (depends on 2)

The antiviral pharmaceutical composition according to claim 2, wherein said anesthetic for local use is selected from the group consisting of lidocaine, xylocaine, bupivacaine, tetracaine, mepivacaine, prilocaine, butacaine, procaine, ropivacaine and mixtures thereof, and is present at a concentration of between 4 and 8% by weight of said antiviral pharmaceutical composition.

### Claim 17 (depends on 1)

A method for treating a virus of a lipid envelop comprising administering a therapeutically effective amount of the antiviral pharmaceutical composition of claim 1, to a subject thereof.

### Claim 18 (depends on 1)

A method for treating Herpes Simplex Virus (HSV) varicella, or herpes zoster virus, said method comprising administering a therapeutically effective amount of the antiviral pharmaceutical composition of claim 1, to a subject in need thereof.
