Cholinergic antagonist patch

• US 5,962,012 A
• Filed: 02/11/1998
• Issued: 10/05/1999
• Est. Priority Date: 11/28/1997
• Status: Expired due to Term

• Current Assignee: Caleb Pharmaceuticals, Inc.
• Original Assignee: Caleb Pharmaceuticals, Inc.
• Inventors: Lin, Wan-Yan, Liao, Chao-Wei, Cheng, Chien-Hsin D., Chen, Shu-Juan
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Berman, Alysia
• Application Number:
  US09/022,308
• Time in Patent Office: 601 Days
• Field of Search: 424/448, 514/946, 514/947, 514/292
• US Class Current: 424/448
• CPC Class Codes: A61K 31/439 the ring forming part of a bridged ring system, e.g. quinuclidine 8-azabicyclo [3.2.1] octanes A61K31/46
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/7061 Polyacrylates

Abstract

Scopolamine is a folksy cholinergic antagonist, and is used by parasympathetic nerves in autonomic nervous neurons as an anti-motion sickness drug or an anti-emesis drug. Since the human body most effectively absorbs this drug through the postauricular skin, the drug is administered by postauricular transdermal resorption patch. The penetrability of drug is increase by adding a dermal penetrative enhancer, because the penetration ability of patch-administered drugs is usually decreased by the penetrative blockade at dermal horny layers. The present invention discloses a penetration enhancer to increase dermal absorption and penetration of the cholinergic antagonist. The present invention finds that polyethylene and amide enhance penetration, about 2.2-2.8 fold. In accordance with the present invention, a penetration enhancer is added to the formulations of transdermal patch to increase the human body'"'"'s absorption of scopolamine.

Claims

1. A formulation for a cholinergic antagonist patch, comprising:

a polyacrylic pressure sensitive adhesive;

scopolamine; and

a penetration enhancer selected from the group consisting of polyethylene glycol glyceryl caprylate and polyethvlene glycol-6 glyceryl mono oleate.

2. A formulation for a cholinergic antagonist patch according to claim 1, wherein the concentration of scopolamine is about 3%-20%.

3. A formulation for a cholinergic antagonist patch according to claim 1, wherein the concentration of the penetration enhancer is about 1%-5%.

4. A formulation for a cholinergic antagonist patch, comprising:

a polyacrylic pressure sensitive adhesive;

scopolamine; and

a penetration enhancer comprising a compound containing 90% lauric acid diethanolamide and 6% diethanolamine.

5. A formulation for a cholinergic antagonist patch according to claim 4, wherein the concentration of the compound is about 2.5%.

6. A formulation for a cholinergic antagonist patch, comprising:

a polyacrylic pressure sensitive adhesive;

scopolamine; and

a penetration enhancer comprising a compound containing 90% coconut fatty acid diethanolamide and 6% diethanolamine.

7. A formulation for a cholinergic antagonist patch according to claim 6, wherein the concentration of the compound is about 2.5%.