Rivastigmine patch for long-term administration

Patent metadata

Field	Value
Publication number	US-12318360-B2
Application number	US-201917271638-A
Country	US
Kind code	B2
Filing date	Aug 30, 2019
Priority date	Aug 31, 2018
Publication date	Jun 3, 2025
Grant date	Jun 3, 2025

Abstract

The present invention relates to a patch comprising a high content of rivastigmine per unit area, which can be continuously administered for a long time. The rivastigmine patch according to the present invention is capable of continuous release of rivastigmine for a long period of time, preferably 3 days, more preferably 4 days or more after attachment, and has excellent physical and chemical stability.

First claim

The invention claimed is:

1. A rivastigmine patch for transdermal treatment comprising a backing film; a rivastigmine matrix layer comprising rivastigmine; a self-adhesive matrix layer comprising an adhesive that adheres to the skin; and a release liner that is removed before use,
wherein the content per patch area of the rivastigmine is 5.4 to 15 mg/cm 2 based on the rivastigmine free base,
the rivastigmine matrix layer comprises a hydrophobic silica,
the self-adhesive matrix layer does not include a rubber-based adhesive polymer, and
the hydrophobic silica comprises silica dimethyl silylate.

2. The rivastigmine patch of claim 1 , wherein the content per patch area of the rivastigmine is 5.4 to 10.8 mg/cm 2 based on the rivastigmine free base.

3. The rivastigmine patch of claim 2 , wherein the content per patch area of the rivastigmine is 5.4 to 9 mg/cm 2 based on the rivastigmine free base.

4. The rivastigmine patch of claim 1 , wherein the content of the hydrophobic silica is 10-50% by weight based on the total weight of the rivastigmine matrix layer.

5. The rivastigmine patch of claim 4 , wherein the rivastigmine matrix layer comprises 10-50% by weight of the rivastigmine, 5-30% by weight of the hydrophobic silica, and 30-80% by weight of an acrylic adhesive based on the total weight of the rivastigmine matrix layer.

6. The rivastigmine patch of claim 5 , wherein the acrylic adhesive is a random copolymer of 58-66 parts by weight of 2-ethylhexyl acrylate, 28-36 parts by weight of methyl acrylate, and 4-8 parts by weight of acrylic acid.

7. The rivastigmine patch of claim 4 , wherein the content per patch area of the rivastigmine is 5.4 to 10.8 mg/cm 2 based on the rivastigmine free base.

8. The rivastigmine patch of claim 4 , wherein the content per patch area of the rivastigmine is 5.4 to 9 mg/cm 2 based on the rivastigmine free base.

9. The rivastigmine patch of claim 1 , wherein the rivastigmine matrix layer further comprises an antioxidant.

10. The rivastigmine patch of claim 1 , wherein the rivastigmine patch comprises a release-controlling membrane that is an ethylene vinyl acetate film between the rivastigmine matrix layer and the self-adhesive matrix layer.

11. The rivastigmine patch of claim 1 , wherein the self-adhesive matrix layer comprises a mixture of two or more silicone adhesives having different physical properties.

12. The rivastigmine patch of claim 1 , wherein the rivastigmine patch is capable of continuous release of rivastigmine for at least 3 days after attachment.

Assignees

• Sk Chemicals Co Ltd

Inventors

• Kim Namho
• Choi Wonjae
• Yoo Hunseung
• Lee Soo Min
• Park Yeo-Jin
• Kim Sung-Hyuk
• Yoo Jong-Su
• Lee Young-Me

Classifications

• A61K47/02

  Inorganic compounds · CPC title

• A61K9/7084 Primary

  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

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K47/24

  containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids · CPC title

• A61K31/27 Primary

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