Effects of Heparin on Topical Use of Plasters Containing a Non-Steroidal Anti-Inflammatory Drug

Patent metadata

Field	Value
Publication number	US-2016243270-A1
Application number	US-201514627036-A
Country	US
Kind code	A1
Filing date	Feb 20, 2015
Priority date	Feb 20, 2015
Publication date	Aug 25, 2016
Grant date	—

Abstract

The present invention provides for a method of improving the release of non-steroidal anti-inflammatory drugs (NSAIDs) from a plaster or bandage comprising an adhesive layer with a pharmaceutically acceptable NSAID together with heparin or a heparinoid. The invention also provides for methods of reducing muscle hyperalgesia in subjects without spontaneous pain.

First claim

We claim:

1 . Method of improving release of non-steroidal anti-inflammatory drugs (NSAIDs) from a bandage comprising:
a) a substrate layer; b) an adhesive layer in the form of a polymeric hydrogel matrix comprising an effective amount of a pharmaceutically acceptable NSAID and heparin or a heparinoid, at least one thickening agent, at least one wetting agent, at least one cross-linking agent; and c) a protective film which can be removed at the moment of use, wherein said hydrogel matrix further comprises a surfactant consisting of sodium ethylenediamine tetraacetate; said method comprising topically applying said bandage to patients in need thereof; and assessing an improved NSAID release compared NSAID release from bandages without heparin.

2 . Method of increasing membrane permeation of non-steroidal anti-inflammatory drugs (NSAID) from a bandage comprising:
a) a substrate layer; b) an adhesive layer in the form of a polymeric hydrogel matrix comprising an effective amount of a pharmaceutically acceptable NSAID and heparin or a heparinoid, at least one thickening agent, at least one wetting agent, at least one cross-linking agent; and c) a protective film which can be removed at the moment of use, wherein said hydrogel matrix further comprises a surfactant consisting of sodium ethylenediamine tetraacetate; said method comprising: applying said bandage to a membrane; and assessing an increased membrane permeation of NSAID compared to membrane permeation obtainable from bandages without heparin.

3 . Method of reducing muscle hyperalgesia in subjects without spontaneous pain, said method comprising:
assessing an initial pain threshold in said subjects; applying to said subjects a bandage comprising:
a) a substrate layer;
b) an adhesive layer in the form of a polymeric hydrogel matrix comprising a pharmaceutically acceptable NSAID and heparin or a heparinoid, at least one thickening agent, at least one wetting agent, at least one cross-linking agent; and
c) a protective film which can be removed at the moment of use, wherein said hydrogel matrix further comprises a surfactant consisting of sodium ethylenediamine tetraacetate;
reassessing the pain threshold; and determining a reduced muscle hyperalgesia in said subjects measured as a difference between the initial and the reassessed pain threshold.

4 . The method according to claim 1 , wherein the NSAID is selected from the group consisting essentially of diclofenac, diflunisal, ibuprofen, ketoprofen, naproxen, acetysalicic acid, salsalate, celecoxib, etodolac, fenoprofen, flurbiprofen, indomethacin, ketorolac, meloxicam, mefenamic acid, nabumetone, oxaprozin, piroxicam, rofecoxib, sulindac, tolmetin, valdecoxib or pharmaceutically acceptable salts thereof.

5 . The method according to claim 1 , wherein the NSAID is diclofenac.

6 . The method according to claim 4 , wherein the diclofenac salt is in the form of a salt with an alicyclic amine of general formula

in which m is 0 or 1.

7 . The method according to claim 4 , wherein the diclofenac salt is the salt of N-hydroxyethyl pyrrolidine.

8 . The method according to claim 1 , wherein the effective amount of NSAID is between 0.1 and 5 wt % with respect to the hydrogel matrix.

9 . The method according to claim 1 , wherein the effective amount of NSAID is between 0.3 and 3 wt % with respect to the hydrogel matrix.

10 . The method according to claim 1 wherein the concentration of heparin or heparinoid is between 0.05 and 1 wt % with respect to the hydrogel matrix.

Assignees

• Altergon Sa

Inventors

• Frangione Valeria
• Lanzarotti Arturo

Classifications

• A61K31/196 Primary

  the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil · CPC title

• A61L2300/802

  Additives, excipients, e.g. cyclodextrins, fatty acids, surfactants · CPC title

• A61F13/00063

  comprising medicaments or additives, e.g. odor control, PH control, debriding, antimicrobic (drug delivery dressings A61K9/70; chemical aspect of the additives A61L15/00) · CPC title

• A61L15/58

  Adhesives · CPC title

• A61L15/28

  Polysaccharides or their derivatives {(A61L15/225 takes precedence)} · CPC title