Anti-inflammatory analgesic patch

• US 5,116,621 A
• Filed: 12/24/1990
• Issued: 05/26/1992
• Est. Priority Date: 12/25/1989
• Status: Expired due to Term

• Current Assignee: Wyeth KK (Pfizer Inc.), Teikoku Seiyaku Co Limited (Teikoku Seiyaku)
• Original Assignee: Lederle (Japan), Ltd. (Pfizer Inc.), Teikoku Seiyaku Co Limited (Teikoku Seiyaku)
• Inventors: Sasaki, Noriyuki, Oji, Akihito, Mizumura, Mitsuo, Tada, Yukihiro
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): HORNE, LEON
• Application Number:
  US07/633,146
• Time in Patent Office: 519 Days
• Field of Search: 424/445, 424/448, 424/449
• US Class Current: 424/445
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• 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
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

An anti-inflammatory analgesic patch having a drug reservoir layer comprising 4-biphenylylacetic acid as the effective ingredient, a homo- and/or co-polymer of acrylic acid and ordinary adjuvants such as a shape-retaining agent, humectant, thickener, etc., which is characterized in that said drug reservoir further contains crotamiton and pH of the drug reservoir is adjusted within a range of 6 to 8 with a water-soluble organic amine and an organic acid.

Claims

1. An anti-inflammatory analgesic dosage unit for transdermal application in the form of a patch having (i) a drug-reservoir layer comprising an effective anti-inflammatory amount of 4-biphenylacetic acid to provide an analgesic effect;

(ii) a polymer of acrylic acid, (iii) at least 0.05 parts by weight crotamiton per 100 parts by weight 4-biphenylacetic acid within said drug-reservoir, and (iv) 0.5 to 15% by weight water-soluble organic amine based on the weight of the drug-reservoir and 0.1 to 5% organic acid based on the weight of the drug-reservoir, said water-soluble organic amine and said organic acid being adjusted whereby said drug-reservoir is maintained at a pH in the range of 6 to 8.

2. The patch of claim 1, in which the water-soluble organic amine is a mono-, di- or tri-(lower alkanolamine).

3. The patch of claim 2, in which the water-soluble organic amine is diisopropanolamine, triethanolamine or diethanolamine.

4. The patch of claim 1, in which the organic acid is selected from malic acid, tartaric acid, citric acid, gluconic acid, lactic acid and oleic acid.

5. The patch of claim 1, in which the pH of the drug reserver is within a range of 6.3 to 7.5.

6. The patch of claim 1 which contains 0.1 to 5% by weight of 4-biphenylylacetic acid based on the weight of the drug reservoir.

7. An anti-inflammatory analgesic patch of claim 1 which includes a humectant.

8. An anti-inflammatory analgesic patch of claim 1 which includes a thickener.

9. An anti-inflammatory analgesic patch of claim 1 wherein said polymer is an acrylic acid homopolyer or copolymer or mixture thereof.