# US 10,765,749 B2 · Non-aqueous patch

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- Number: US 10,765,749 B2
- Document ID: US10765749B2
- Status: Granted
- Kind: B2
- Application number: 15/891,915
- Filed: 2018-02-08
- Published: 2018-11-15
- Granted: 2020-09-08
- Earliest claimed: 2016-03-09
- Assignees: ITOCHU CHEMICAL FRONTIER Corporation; Oishi Koseido Co., Ltd.
- Applicants: Itochu Chemical Frontier Corporation; Oishi Koseido Co., Ltd.
- Inventors: Tatsuya Mori; Naoyuki Saida
- Web page: https://patentgrep.com/patent/US10765749B2

## CPC

- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 9/7053: {obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- 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)

## Abstract

Non-aqueous patches comprising lidocaine, which is not dissolved and is present in a crystalline state, have poor permeability to the skin. Therefore, non-aqueous patches have a high concentration of lidocaine. It is pointed out that lidocaine has an adverse effect on the heart. Prolonged use of a high concentration of lidocaine causes side effects, such as shock, rubor, and irritating sensation. External preparations comprising more than 5 mass % of lidocaine are designated as powerful drugs, and cannot be used as household (nonprescription) medicine. Provided is a non-aqueous patch that is effective to relieve muscle pain, the non-aqueous patch comprising lidocaine and/or its reactant, and a dissolving agent composed of an organic acid and a polyalcohol, which are contained in a base.

## Claims

### Claim 1

A non-aqueous patch comprising a plaster comprising lidocaine, a dissolving agent, and an elastomer, wherein, the plaster comprises 0.5 to 7 mass % lidocaine and 1.435 to 9.1 mass% dissolving agent, the dissolving agent comprises dipropylene glycol and isostearic acid, and the isostearic acid is present in the plaster in an amount of 1.4 to 2.1 mass%.

### Claim 2 (depends on 1)

The non-aqueous patch according to claim 1, wherein the elastomer consists of polyisobutylene and styrene isoprene rubber.

### Claim 3 (depends on 1)

The non-aqueous patch according to claim 1, wherein the plaster comprises 10 mass % to 40 mass % of the elastomer.

### Claim 4 (depends on 1)

The non-aqueous patch according to claim 1, wherein the plaster comprises 20 mass % to 40 mass % of the elastomer.

### Claim 5 (depends on 1)

The non-aqueous patch according to claim 1, wherein the plaster further comprises a terpene resin.

### Claim 6 (depends on 1)

The non-aqueous patch of claim 1, wherein after application to a human for 12 hours, the amount of lidocaine remaining in the non-aqueous patch is 80% or less than the amount prior to application.