Patch containing rivastigmine

Patent metadata

Field	Value
Publication number	US-9585862-B2
Application number	US-201214118985-A
Country	US
Kind code	B2
Filing date	May 21, 2012
Priority date	May 20, 2011
Publication date	Mar 7, 2017
Grant date	Mar 7, 2017

Abstract

The present invention relates to a rivastigmine-containing patch having improved storage stability and proper release property.

First claim

What is claimed is:

1. A rivastigmine-containing patch, comprising:
(a) a drug-containing adhesive layer comprising rivastigmine free base, a copolymer of butyl methacrylate and methyl methacrylate, and an adhesive; and
(b) a layer for adhering to the skin comprising a silicon adhesive,
wherein the adhesive in the drug-containing adhesive layer is a random copolymer of 58 to 66 parts by weight of 2-ethylhexyl acrylate, 28 to 36 parts by weight of methyl acrylate and 4 to 8 parts by weight of acrylic acid, and
wherein the drug-containing adhesive layer and the layer for adhering to the skin do not contain tocopherol.

2. The rivastigmine-containing patch of claim 1 , wherein the adhesive in the drug-containing adhesive layer has a solids content of 36.5%, a Brookfield viscosity value of 8000 mPa·s, a density of 0.92 g/ml, and a solvent composition comprising 87% ethyl acetate and 13% hexane.

3. The rivastigmine-containing patch of claim 1 , wherein the copolymer of butyl methacrylate and methyl methacrylate is a random copolymer thereof, and has a weight average molecular weight of 130,000 g/mol to 170,000 g/mol.

4. The rivastigmine-containing patch of claim 3 , wherein the copolymer of butyl methacrylate and methyl methacrylate has a weight average molecular weight of about 150,000 g/mol.

5. The rivastigmine-containing patch of claim 1 , wherein the silicon adhesive is trimethylated silica treated with dimethyl siloxane.

6. The rivastigmine-containing patch of claim 5 , wherein the silicon adhesive has a viscosity of 1200 mPa·s, a solid content of 60%, and a peel adhesion value of 700 g/cm.

7. The rivastigmine-containing patch of claim 6 , wherein the silicon adhesive is used in an amount of 27 mg/10 cm 2 to 33 mg/10 cm 2 based on the dry weight of the layer for adhering to the skin.

8. A product comprising a rivastigmine-containing patch, wherein the rivastigmine-containing patch of claim 1 is packaged by nitrogen filling.

9. A product comprising a rivastigmine-containing patch, wherein the rivastigmine-containing patch of claim 3 is packaged by nitrogen filling.

10. A product comprising a rivastigmine-containing patch, wherein the rivastigmine-containing patch of claim 5 is packaged by nitrogen filling.

11. A product comprising a rivastigmine-containing patch, wherein the rivastigmine-containing patch of claim 7 is packaged by nitrogen filling.

12. The rivastigmine-containing patch of claim 1 , wherein the adhesive in the drug-containing adhesive layer has a solids content of 36.5%, a Brookfield viscosity value of 8000 mPa·s, a density of 0.92 g/ml, and a solvent composition comprising 87% ethyl acetate and 13% hexane,
wherein the copolymer of butyl methacrylate and methyl methacrylate is a random copolymer thereof, and has a weight average molecular weight of 130,000 g/mol to 170,000 g/mol, and
wherein the silicon adhesive is trimethylated silica treated with dimethyl siloxane.

13. The rivastigmine-containing patch of claim 12 , wherein the silicon adhesive has a viscosity of 1200 mPa·s, a solid content of 60%, and a peel adhesion value of 700 g/cm.

14. The rivastigmine-containing patch of claim 12 , wherein the silicon adhesive is used in an amount of 27 mg/10 cm 2 to 33 mg/10 cm 2 based on the dry weight of the layer for adhering to the skin.

Assignees

• Hwang Yong-Youn
• Choi Won-Jae
• Kim Jae-Sun
• Youn Won-No
• Park Yeo-Jin
• Oh Joon-Gyo
• Im Jongseob
• Sk Chemicals Co Ltd

Inventors

• Hwang Yong-Youn
• Choi Won-Jae
• Kim Jae-Sun
• Youn Won-No
• Park Yeo-Jin
• Oh Joon-Gyo
• Im Jongseob

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61L15/58

  Adhesives · CPC title

• A61K31/27

  of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine · CPC title

• A61K31/325 Primary

  Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof (thiurams A61K31/145) · CPC title

• A61K9/7084

  Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches · CPC title