Transdermal absorption of active substances from subcooled melts

• US 6,344,211 B1
• Filed: 11/21/2000
• Issued: 02/05/2002
• Est. Priority Date: 12/24/1994
• Status: Expired due to Term

• Current Assignee: Purdue Pharma L.P.
• Original Assignee: LTS Lohmann Therapie-Systeme GmbH
• Inventors: Hille, Thomas
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): CHANNAVAJJALA, LAKSHMI SARADA
• Application Number:
  US09/716,442
• Time in Patent Office: 441 Days
• Field of Search: 424/447, 424/448, 424/449, 514/946, 514/567
• US Class Current: 424/449
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7061 Polyacrylates

Abstract

A pharmaceutical product for the release of medicinal agents to the skin having absorption-increasing auxiliary agents is characterized in that the auxiliary material forms subcooled melts.

Claims

1. A method of releasing a pharmaceutical agent for effecting a topical or systemic effect in a patient from a transdermal therapeutic system having a layered structure and comprising at least one substance selected from the group of pharmaceutical agents producing a local or systemic effect and at least one auxiliary agent which increases the penetration of said pharmaceutical agents and has a melting point above room temperature, which comprises:

a) in a first step preparing said transdermal therapeutic system by using an auxiliary agent which has been melted and afterwards allowed to form a subcooled melt by cooling it down to room temperature, and

b) in a second step applying the transdermal therapeutic system as prepared in the first step on the skin of said patient.

2. The method according to claim 1, wherein the pharmaceutical agent producing a local effect is a member selected from the group consisting of antiperspirants, fungicides, bactericides, and bacteriostatics.

3. The method according to claim 1, wherein the pharmaceutical agent producing a systemic effect is a member selected from the group consisting of antibiotics, hormones, antipyretics, antidiabetic agents, coronary vasodilators, cardioactive glycosides, analgetics, spasmolytics, antihypertensives, psychotropic drugs, migraine analgesics, corticoids, contraceptives, antirheumatics, anticholinergics, symphaticolytics, symphaticomimetics, vasodilators, anticoagulants, and antiarrhytmics.

4. The method according to claim 1, wherein the pharmaceutical agent producing a systemic effect is a member selected from the group consisting of buprenorphine base, pilocarpine base, and ephedrine base.

5. The method according to claim 1, wherein the pharmaceutical agent is buprenorphine base and the auxiliary agent is selected from the group consisting of levulic acid, glutaric acid monomethyl ester and dodecanol.

6. The method according to claim 1, wherein the pharmaceutical agent is buprenorphine base and the auxiliary agent is levulic acid.