Transdermal patch containing Rotigotine

Patent metadata

Field	Value
Publication number	US-9265752-B2
Application number	US-66791508-A
Country	US
Kind code	B2
Filing date	Jul 3, 2008
Priority date	Jul 6, 2007
Publication date	Feb 23, 2016
Grant date	Feb 23, 2016

Abstract

A Rotigotine-containing composition having a matrix mixture system formed from a polyvinylpyrrolidone and a combination of an acrylic pressure-sensitive adhesive with a silicone pressure-sensitive adhesive. The polyvinylpyrrolidone may be present in an amount of about 1-10% by weight in matrix mixture system. The acrylic pressure-sensitive adhesive may be present in an amount of about 1-25% by weight in the matrix mixture system. The silicone pressure-sensitive adhesive may be present in an amount of about 65-98% by weight in the matrix mixture system. The composition further includes 1-40% of Rotigotine on the basis of the total weight of the composition. The composition provides improved properties in the solubility, release and initial penetration level of Rotigotine. Also disclosed is a transdermal patch that includes the Rotigotine-containing composition, as well as methods of manufacturing and using the Rotigotine-containing composition.

First claim

The invention claimed is:

1. A rotigotine-containing transdermal patch comprising a matrix layer composition,
wherein the matrix layer composition comprises, on the basis of the total weight of the matrix layer composition, 79-84% by weight of a matrix mixture system and 8-11% by weight of rotigotine,
wherein the matrix mixture system is formed from a combination of a first adhesive comprising an acrylate copolymer with a second adhesive comprising dimethyl silicone polymers and silicone resins, and polyvinylpyrrolidone, wherein
(1) the first adhesive is present in an amount of 5-15% by weight in the matrix mixture system,
(2) the second adhesive is present in an amount of 65-75% by weight in the matrix mixture system, and
(3) the polyvinylpyrrolidone is present in an amount of 1-1.5% by weight in the matrix mixture system;
wherein the rotigotine is in the form of the free base or a pharmaceutically acceptable salt,
wherein the acrylate copolymer is copolymerized from monomer units selected from the group consisting of butyl acrylate, isooctyl acrylate, vinyl acetate, acrylamide, and α-methacrylic acid,
wherein the 0-12 hour accumulative release amount of rotigotine is about 210 to about 226 μg/cm 2 ,
wherein the matrix layer composition further comprises at least one auxiliary selected from the group consisting of permeation enhancers and antioxidants, and wherein if the permeation enhancer is present, the permeation enhancer is present in an amount of 8-10% based on the total weight of the matrix layer composition.

2. The rotigotine-containing transdermal patch of claim 1 , wherein the permeation enhancer is selected from the group consisting of surfactants, alcohols, polyols, esters, dimethyl sulfoxide, fatty acids, fatty alcohols, fatty acid esters, azones, N methylpyrrolidone, 1,5-dimethylpyrrolidone, 5-carboxylpyrrolidone, salicylic acid, and terpenes.

3. The rotigotine-containing transdermal patch of claim 1 , wherein the antioxidant is selected from the group consisting of vitamin E, ascorbyl palmitate, sodium metasulfite and mixtures thereof.

4. The rotigotine-containing transdermal patch of claim 1 , wherein the permeation enhancer is selected from the group consisting of isopropyl myristate, lauryl acid and N-methylpyrrolidone.

5. The rotigotine-containing transdermal patch of claim 1 , wherein the acrylate copolymer comprises butyl acrylate monomer units.

6. The rotigotine-containing transdermal patch of claim 1 , wherein the acrylate copolymer comprises isooctyl acrylate monomer units.

7. The rotigotine-containing transdermal patch of claim 1 , wherein the acrylate copolymer comprises vinyl acetate monomer units.

8. The rotigotine-containing transdermal patch of claim 1 , wherein the acrylate copolymer comprises acrylamide monomer units.

9. The rotigotine-containing transdermal patch of claim 1 , wherein the acrylate copolymer comprises α-methacrylic acid monomer units.

10. The rotigotine-containing transdermal patch of claim 1 , wherein the acrylate copolymer comprises butyl acrylate, isooctyl acrylate, vinyl acetate, acrylamide, and α-methacrylic acid monomer units.

11. The rotigotine-containing transdermal patch of claim 1 , wherein the second adhesive is a pressure-sensitive adhesive.

12. The rotigotine-containing transdermal patch of claim 1 , wherein the matrix mixture system is saturated with rotigotine.

Assignees

• Wang Shuming
• Xue Huiyong
• Wang Li
• Zhang Enhong
• Lian Hongjun
• Shi Xiaoyan
• Chi Guohua
• Lu Yucheng
• Liu Xiquan
• Song Li
• Zhong Xuying
• Du Hongguang
• Jiangsu Kangbeide Pharmaceuticals Co Ltd

Inventors

• Wang Shuming
• Xue Huiyong
• Wang Li
• Zhang Enhong
• Lian Hongjun
• Shi Xiaoyan
• Chi Guohua
• Lu Yucheng
• Liu Xiquan
• Song Li
• Zhong Xuying
• Du Hongguang

Classifications

• A61P25/16

  Anti-Parkinson drugs · CPC title

• A61P25/24

  Antidepressants · CPC title

• A61P25/14

  for treating abnormal movements, e.g. chorea, dyskinesia · CPC title

• A61P25/18

  Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia · CPC title

• A61K9/7053 Primary

  obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene · CPC title