Transdermal drug-delivery composition

• US 4,906,463 A
• Filed: 04/08/1988
• Issued: 03/06/1990
• Est. Priority Date: 12/22/1986
• Status: Expired due to Term

• Current Assignee: Ortho-McNeil Pharmaceutical Incorporated (Johnson & Johnson)
• Original Assignee: Cygnus Research Corporation
• Inventors: Cleary, Gary W., Roy, Samir
• Primary Examiner(s): Schenkman, Leonard
• Application Number:
  US07/179,423
• Time in Patent Office: 697 Days
• Field of Search: 514/552, 514/967, 514/785, 514/182, 514/329, 424/78
• US Class Current: 424/449
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 9/703 characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
• 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

Abstract

A solid state, resilient laminated composite for administering a drug transdermally consisting of a multiplicity of spaced structural laminas of a resilient elastomer, one of which forms the top of the composite, a viscoelastic hydrophobic polymer lamina containing propylene glycol monolaurate interposed between each structural lamina and a pressure-sensitive adhesive lamina that provides the basal surface of the composite and consists of a blend of a pressure-sensitive adhesive, drug and propylene glycol monoalaurate.

Claims

1. A pharmaceutical composition for transdermal or transmucosal administration comprising a nonaqueous mixture of a polymer, a drug and a permeation enhancing amount of a fatty acid ester or fatty alcohol ether of a C₂ to C₄ alkanediol where each fatty acid or fatty alcohol portion of the ester or ether is of about 8 to 22 carbon atoms.

2. The pharmaceutical composition of claim 1 wherein the composition is in the form of a solid state transdermal drug delivery device.

3. The pharmaceutical composition of claim 2 wherein the drug is estradiol or fentanyl.

4. The pharmaceutical composition of claim 2 wherein the device is a laminated composite of a reservoir layer and a pressure sensitive adhesive layer.

5. The pharmaceutical composition of claim 4 wherein the drug and the fatty acid ester or fatty alcohol ether are both contained primarily in the reservoir layer.

6. The pharmaceutical composition of claim 1 wherein the ester is a monoester and the ether is a monoether.

7. A pharmaceutical composition for transdermal or transmucosal administration comprising a nonaqueous mixture of a polymer, a drug and a permeation enhancing amount of a fatty acid monoester of propylene glycol.

8. The pharmaceutical composition of claim 7 wherein the fatty acid monoester of propylene glycol is propylene glycol monolaurate.

9. The pharmaceutical composition of claim 8 wherein the drug is estradiol or fentanyl.

10. A method of enhancing the permeation of a body surface to a drug administered to the surface comprising coadministering to the surface a permeation enhancing amount of a fatty acid ester or a fatty alcohol ether of a C₂ to C₄ alkanediol where each fatty acid or fatty alcohol portion of the ester or ether is of about 8 to 22 carbon atoms and wherein said ester or ether is administered from a nonaqueous mixture comprising a polymer and said ester or ether.

11. The method of claim 10 wherein the drug is estradiol or fentanyl.

12. A method of enhancing the permeation of skin to estradiol or fentanyl comprising coadministering to the skin a permeation enhancing amount of propylene glycol monolaurate from a nonaqueous mixture of estradiol or fentanyl, a polymer, and propylene glycol monolaurate.