# US 8,771,724 B2 · Percutaneous absorption enhancer and transdermal preparation using the same

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- Number: US 8,771,724 B2
- Document ID: US8771724B2
- Status: Granted
- Kind: B2
- Application number: 13/000,635
- Filed: 2009-06-22
- Published: 2011-05-05
- Granted: 2014-07-08
- Earliest claimed: 2008-06-23
- Assignees: Toa Eiyo Ltd.
- Applicants: Naoto Ohtake; Yuuki Koide
- Inventors: Naoto Ohtake; Yuuki Koide
- Web page: https://patentgrep.com/patent/US8771724B2

## CPC

- A61K 9/7053: {obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene}
- 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 9/7061: {Polyacrylates}
- A61K 9/7069: {obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide}
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic 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
- A61P 7/12: Antidiuretics, e.g. drugs for diabetes insipidus (ADH A61P5/10)
- A61P 9/12: Antihypertensives
- A61P 25/22: Anxiolytics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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

Provided are a percutaneous absorption enhancer excellent in an enhancing effect on percutaneous absorption of a wide range of drugs and excellent in compatibility with an adhesive base, and a transdermal preparation using the percutaneous absorption enhancer. The percutaneous absorption enhancer includes a sulfosuccinate or a salt thereof and an alkyl glycoside or an alkyl thioglycoside.

## Claims

### Claim 1

A matrix-type transdermal preparation, comprising:
a tape comprising drug containing layers comprising an adhesive base,
a percutaneous absorption enhancer comprising 0.01 to 10% of a sulfosuccinate or a salt thereof and 0.01 to 10% of an alkyl glycoside or an alkyl thioglycoside, wherein the sulfosuccinate or a salt thereof and the alkyl glycoside or the alkyl thioglycoside are present in a total amount of from 0.1 to 20%; and
a drug.

### Claim 2 (depends on 1)

The matrix-type transdermal preparation according to claim 1, wherein the sulfosuccinate or the salt thereof is a C6-C18 dialkyl sulfosuccinate or a salt thereof.

### Claim 3 (depends on 1)

The matrix-type transdermal preparation according to claim 1, wherein the alkyl glycoside or the alkyl thioglycoside is a C6-C18 alkyl glycoside or a C6-C18 alkyl thioglycoside.

### Claim 4 (depends on 1)

The matrix-type transdermal preparation according to claim 1, wherein the sulfosuccinate or the salt thereof is a dioctyl sulfosuccinate or a salt of the dioctyl sulfosuccinate.

### Claim 5 (depends on 1)

The matrix-type transdermal preparation according to claim 1, wherein the alkyl glycoside or the alkyl thioglycoside is an n-octyl-β-D-thioglucopyranoside or an n-dodecyl-β-D-glucopyranoside.

### Claim 6 (depends on 1)

The matrix-type transdermal preparation according to claim 1, wherein each of the drug containing layers comprises an adhesive base, the drug, and the percutaneous absorption enhancer laminated on one surface of a supporting sheet.

### Claim 7 (depends on 6)

The matrix-type transdermal preparation according to claim 6, wherein the adhesive base consists of an acrylic adhesive base, a rubber-based adhesive base, or a silicone-based adhesive base.

### Claim 8 (depends on 1)

The matrix-type transdermal preparation according to claim 1, wherein the drug is a compound having a carboxyl group or a bioisoster thereof and an aliphatic amino group and/or an aromatic amino group.

### Claim 9

A method of enhancing percutaneous absorption of a drug, the method comprising transdermally administering a matrix-type transdermal tape preparation comprising the drug with a percutaneous absorption enhancer comprising 0.01 to 10% of a sulfosuccinate or a salt thereof, and 0.01 to 10% of an alkyl glycoside or an alkyl thioglycoside, wherein the sulfosuccinate or a salt thereof and the alkyl glycoside or the alkyl thioglycoside are present in a total amount of from 0.1 to 20%.

### Claim 10 (depends on 9)

The method according to claim 9, wherein the drug and the sulfosuccinate or a salt thereof, and an alkyl glycoside or an alkyl thioglycoside are in the matrix-type transdermal tape preparation.

### Claim 11 (depends on 9)

The method according to claim 9, wherein the matrix type transdermal tape preparation comprises drug-containing layers, wherein each of the drug containing layers comprises an adhesive base, the drug, and the percutaneous absorption enhancer laminated on one surface of a supporting sheet.

### Claim 12 (depends on 11)

The method according to claim 11, wherein the adhesive base consists of an acrylic adhesive base, a rubber-based adhesive base, or a silicone-based adhesive base.

### Claim 13 (depends on 9)

The method according to claim 9, wherein the drug is a compound having a carboxyl group or a bioisoster thereof and an aliphatic amino group and/or an aromatic amino group.

### Claim 14 (depends on 1)

The matrix-type transdermal preparation according to claim 1, wherein the adhesive base is alkyl acrylate adhesive.