# US 10,765,640 B2 · Non-aqueous patch

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- Number: US 10,765,640 B2
- Document ID: US10765640B2
- Status: Granted
- Kind: B2
- Application number: 14/346,794
- Filed: 2011-09-27
- Published: 2014-12-04
- Granted: 2020-09-08
- Earliest claimed: 2011-09-27
- Assignees: ITOCHU CHEMICAL FRONTIER Corporation; Oishi Koseido Co., Ltd.
- Applicants: Tatsuya Mori; Naoyuki Saida
- Inventors: Tatsuya Mori; Naoyuki Saida
- Web page: https://patentgrep.com/patent/US10765640B2

## CPC

- A61K 9/7038: {Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer}
- 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
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 23/02: Local anaesthetics
- 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

[Problem] If lidocaine is composed of non-aqueous patch, the adhesive power of the preparation tends to get lower, as the composition amount of lidocaine is higher. It is popular to solve lidocaine in dissolving agent in order to compose lidocaine in patch and release effective amount into skin. However, if the amount of dissolving agent gets higher, the adhesive power gets extremely lower, so that an long-time attachment is difficult. [Solution] A non-aqueous patch comprising lidocaine and/or its reactant, and a dissolving agent which are contained in a base of plaster, the plaster being hold by a support, of which strength of 50% stretched to longitudinal direction is less than 2,000 g/50 mm and of biaxially-oriented stretch cloth.

## Claims

### Claim 1

A non-aqueous patch comprising 0.5 to 7 mass % lidocaine, and a dissolving agent comprising an organic acid and a polyalcohol, wherein the lidocaine and the dissolving agent are in a plaster, the plaster being held by a support, wherein the support has a stretch strength of less than 2,000g/50 mm when the support is stretched by 50% longitudinal extension; and wherein the support comprises a biaxially-oriented stretch cloth, wherein
the organic acid is isostearic acid, which is present in the plaster in an amount of 0.9 mass % to 2.5 mass %, and
the polyalcohol is dipropylene glycol, which is present in the plaster in an amount of 0.2 mass % to 1.5 mass % dipropylene glycol.

### Claim 2 (depends on 1)

The non-aqueous patch of claim 1, wherein the adhesive power of the patch is from 0.4N/width 25 mm to 5N/width 25 mm.

### Claim 3 (depends on 1)

The non-aqueous patch of claim 1, wherein the release ratio of lidocaine from the plaster is more than 6%, after 12 hours attachment to the skin.

### Claim 4 (depends on 1)

The non-aqueous patch of claim 1, wherein the amount of lidocaine is 0.1 to 1 mg/cm2 of the plaster.

### Claim 5 (depends on 1)

The non-aqueous patch of claim 1, wherein the plaster consists of lidocaine, isostearic acid and dipropylene glycol, an elastomer, a terpene resin, butylated hydroxytoluene, liquid paraffin and light anhydrous silicic acid.

### Claim 6 (depends on 5)

The non-aqueous patch of claim 5, wherein
the elastomer consists of a combination of styrene isoprene and polyisobutylene.

### Claim 7 (depends on 1)

The non-aqueous patch of claim 1, wherein the lidocaine is dissolved in the dissolving agent.

### Claim 8 (depends on 5)

The non-aqueous patch of claim 5, wherein the lidocaine, the polyalcohol and the organic acid are combined prior to the addition of the elastomer, the terpene resin, the butylated hydroxytoluene, the liquid paraffin and the light anhydrous silicic acid.