Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Reexamination Certificate
1997-06-27
2001-02-20
Clardy, S. Mark (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
C424S448000, C602S041000, C604S289000, C604S304000, C604S305000, C604S307000
Reexamination Certificate
active
06190690
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a ketoprofen patch appropriate in treating arthritis, and more particularly to a remedy containing ketoprofen, which is percutaneously administrated and has therapeutic effect on arthritis, rheumatism, etc.
2. Description of the Prior Art
Ketoprofen plaster (trade name; KETOTOP, Pacific Pharm. Co., Ltd.) sold at the market as an arthritis remedy which is percutaneously administrated, consists of nonwoven fabric, poly(isobutylene) rubber adhesive as a primer, which is formed on the nonwoven fabric by transfer coating, and mixture of acrylic adhesive, ketoprofen as drug and propylene glycol monolaurate as an enhancer for helping permeation of the drug into skin, which is formed on the primer by transfer coating. Thus manufactured ketoprofen plaster rarely has any difference with the conventional PAS (para-aminosalicylic acid) agent.
U.S. Pat. No. 5,505,956 discloses a ketoprofen patch having 2-5 adhesion layers between a backing as a supporting material and a liner. In the ketoprofen patch, when a non-moisture-permeable backing is used, layers from the backing to a surface layer which is to be contacted with skin, consist of from a layer having a high moisture content to a layer having a low moisture content. On the contrary, when a moisture-permeable backing such as nonwoven fabric is used, layers from the backing to the surface layer which is to be contacted with the skin, consist of from a layer having a low moisture content to a layer having a high moisture content. In order to increase moisture content, the ketoprofen patch uses 0.3-30 wt % of poly(vinyl alcohol), and in each layer, 0.1-40 wt % of ketoprofen is mixed with acrylic adhesive and an enhancer such as propylene monoglycolate.
However, in the ketoprofen patch constructed as mentioned above, since ketoprofen drug exists as a mixture with the acrylic adhesive, even though solubility of ketoprofen is good, diffusion thereof is to be late. In addition, since the release amount of the drug can not be controlled, the amount of drug administered cannot be kept constant over of time. Further, since the ketoprofen which is pulverulent drug, or a non-adhesive type polymer such as the poly(vinyl alcohol) are mixed with the acrylic adhesive, the adhesion strength to the skin is so flimsy that re-attachment of the patch to the skin becomes difficult.
Particularly, because the patch is a medium for transferring drug through the skin, therapeutic effect is proportional to contacting area between the patch and the skin. Therefore, if the area of the patch peeled off from the skin is wide, the drug transferance rate decreases and accordingly, the therapeutic effect remarkably decreases.
Hence, development for a ketoprofen patch having a good adhesion strength for keeping therapeutic effect of drug for a long time, a constant drug release amount per unit time and a good initial drug release characteristic, is highly demanded in this technical field.
SUMMARY OF THE INVENTION
The present invention has thus been constructed to overcome one or more of the above described problems of the conventional art. Accordingly, it is an object of the present invention to provide a sustained/immediate acting ketoprofen patch which can control the drug release amount whereby therapeutic effect of the patch can be continuously and homogeneously or immediately kept.
Another object of the present invention is to provide a sustained/immediate acting ketoprofen patch having a good adhesion strength to skin whereby the therapeutic effect of the patch can sufficiently be transferred to the skin when the patch is attached to the skin, and attaching/detaching of the patch to/from the skin can be possible as occasion needs.
Still another object of the present invention is to provide a ketoprofen patch having a continuously constant drug release effect or a good initial drug release effect.
Yet another object of the present invention is to provide a method for rid manufacturing the above mentioned sustained/immediate acting ketoprofen patch.
To accomplish the object of the present invention, there is provided a sustained/immediate acting ketoprofen patch comprising: a backing; a non-moisture-permeable acrylic/rubber adhesive primer; a high-moisture-permeable drug layer in which ketoprofen is dissolved in water soluble polymer; and a skin adhesion layer capable of controlling release amount of a drug. Particularly, the ketoprofen patch has a complex laminated-structure in which the drug layer and an adhesive layer are completely separated.
In the present invention, the term, “non-moisture-permeable” means hardly permeating moisture, and the term of “high-moisture-permeable” means permeating moisture very well.
Methods for manufacturing the ketoprofen patches of the sustained type or the immediate acting type are similar but different only in employing materials according to the types.
The sustained ketoprofen patch from which drug is continuously released with the lapse of time is manufactured by a method comprising the steps of: (1) forming a primer by coating an acrylic adhesive dissolved in ethyl acetate onto a silicon coated paper or a polyester film, drying at 80° C. for 1-2 minutes (thickness of a coating layer is 20-50 &mgr;m), and then transfer coating onto a backing; (2) forming a drug layer by coating a drug solution prepared by adding ketoprofen dissolved in an enhancer to a mixture of an aqueous PVA and an adhesive of acrylic emulsion, and/or EVA emulsion, and/or synthetic rubber latex, onto a silicon coated paper, drying (thickness of a coating layer is 30-50 &mgr;m), and transfer coating onto the printer; and (3) forming a skin adhesion layer by dissolving an emulsifier in ethyl acetate to obtain a solution, mixing the solution with an acrylic adhesive, stirring the thus obtained mixture, coating onto a silicon coated paper, drying (thickness of coating layer is 5-40 &mgr;m, preferably 10-20 &mgr;m), and transfer coating onto the drug layer.
The immediate acting ketoprofen patch having a good initial release effect of drug is manufactured by another method comprising the steps of: (1) forming a primer by coating a rubber adhesive onto a silicon coated paper or polyester film, drying at 60° C. for 1-2 minutes and at 80° C. for 1 minute (thickness of coating layer is 20-50 &mgr;m, preferably 30-40 &mgr;m), and transfer coating onto a moisture-permeable backing; (2) forming a drug layer by coating a drug solution prepared by mixing ethylene-vinyl acetate copolymer emulsion and/or synthetic rubber latex in aqueous PVA, and adding ketoprofen dissolved in an enhancer, onto a silicon coated paper, dying (thickness of coating layer is 10-100 &mgr;m, preferably 30-40 &mgr;m), and transfer coating onto the primer; (3) forming a skin adhesive layer by dissolving emulsifier in ethyl acetate to obtain a solution, mixing the solution with an acrylic adhesive, stirring the mixture, coating onto a silicon coated paper, drying (thickness of coating layer is 5-40 &mgr;m, preferably 10-20 &mgr;m), and transfer coating onto the drug layer.
The immediate acting ketoprofen patch according to the present invention can maximally restrain a reverse diffusion of the drug and the enhancer to the primer, through action of the rubber adhesive contained in the primer, and can accomplish the smooth release of the drug by increasing hydrophobicity of the drug layer by adding the EVA or the synthetic rubber latex to a water soluble polymer.
Most of the percutaneous absorbable agent is, except a type having drug layer of liquid phase such as reservoir type or hydrogel type, used polymer having adhesion or adhesive property as a binder in case of a matrix type having a drug layer of solid phase such as the present invention. However, in the present invention, a binder having no adhesion or adhesive property can be used, so that selection range of the binder becomes broad.
REFERENCES:
patent: 5505956 (1996-04-01), Kim et al.
patent: 5730999 (1998-03-01), Lehmann et al.
Choi Jae-Keun
Ha Yi-Dan
Hyun Byong-Chul
Lee Kwang-Ho
Park Chang-Kyu
Clardy S. Mark
Cook Alex McFarron Manzo Cummings & Mehler, Ltd.
STC Corporation
Williamson Michael A.
LandOfFree
Sustained/immediate acting ketoprofen patch and process for... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Sustained/immediate acting ketoprofen patch and process for..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Sustained/immediate acting ketoprofen patch and process for... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2608693