Transdermal patch for delivering volatile liquid drugs

• US 6,974,588 B1
• Filed: 12/07/1999
• Issued: 12/13/2005
• Est. Priority Date: 12/07/1999
• Status: Expired due to Fees

• Current Assignee: AGI Therapeutics Research Limited
• Original Assignee: Elan Pharma International Limited (Perrigo Company PLC)
• Inventors: Betlach, Charles J. II, Miranda, Jesus
• Primary Examiner(s): Kishore, Gollamudi S.
• Assistant Examiner(s): GHALI, ISIS A D
• Application Number:
  US09/456,278
• Time in Patent Office: 2,198 Days
• Field of Search: 424/448, 424/449, 424/443, 514/343
• US Class Current: 424/448
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/465 Nicotine; Derivatives thereof
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61K 9/7069 obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide
• CPC Class Codes: A61K 9/7092 Transdermal patches having multiple drug layers or reservoirs, e.g. for obtaining a specific release pattern, or for combining different drugs

Abstract

A transdermal patch for administering a volatile liquid drug, such as nicotine, transdermally to a patient comprising a four-layer laminated composite of: a top drug impermeable backing layer; a pressure sensitive silicone adhesive layer containing the drug; a pressure sensitive acrylic adhesive layer also containing the drug; and a removable siliconized release liner layer. Also disclosed is a method for treating a person for nicotine dependence and particularly for treating a woman for nicotine dependence.

Claims

1. A transdermal patch for administering a volatile liquid drug transdermally to a patient comprising

a) a top backing layer that is impermeable to the drug;

b) an intermediate, cast, amine-compatible solid silicone adhesive layer which underlies the backing layer, has a thickness of from about 25 microns to about 100 microns, and contains from about 5 to about 50 wt. % of the drug based on the total dry weight of the drug and adhesive, and is a source in the patch of the drug;

c) a solid acrylic adhesive layer having a thickness of from about 25 microns to about 100 microns and comprising a copolymer of (i) vinyl acetate, (ii) acrylic acid, and (iii) at least one monomer selected from the group consisting of acrylate and methacrylate, and which underlies and is in diffusional contact with the silicone adhesive layer; and

d) a removable release liner layer underlying the acrylic adhesive layer, wherein the relative thickness of layers “

b” and

“

c”

, and the concentration of drug initially present in layer “

b”

is selected to provide a drug flux profile which is characterized by an initial period during which the flux rises to a level suitable for administering a therapeutic amount of the drug, and a second period during which the drug flux is sustained above said level, said second period lasting for at least twice as long as said initial period, and wherein the amount of drug in the patch is sufficient to provide a therapeutically effective amount of drug to the patient over a period of at least about several hours and wherein the drug is a combination of nicotine and mecamylamine and the patch is capable of administering 0.2 to 1.5 mg nicotine per hour and 0.02 to 1 mg mecamylamine per hour to the patient.

2. The patch of claim 1, wherein the silicone adhesive layer comprises a silicone pressure sensitive adhesive.

3. The patch of claim 1, wherein the patch contains an amount of drug sufficient to provide administration of the drug for a period of up to about 72 hours.