Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Matrices
Reexamination Certificate
2001-02-08
2004-05-11
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Matrices
C424S400000, C424S486000, C424S487000, C424S448000
Reexamination Certificate
active
06733785
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a percutaneous absorption preparation, more particularly to a reservoir type percutaneous absorption preparation wherein at the time of preservation a permeation controlling film is in-permeable to medicines and the medicines exist stably in a medicine storage layer and wherein at the time of application of the preparation, as the permeation controlling film is plasticized by moisture evaporating from the skin, the medicines move into a layer of an adhesive and are absorbed through the skin.
BACKGROUND ART
As a conventional percutaneous absorption preparation there is reported a system in which a medicine storage layer and a medicine activating agent are divided by a medicine in-permeable film and, with the in-permeable film being made destroyed or burst by the user upon application, the medicine moves to a layer of an adhesive by the aid of the activating agent and is absorbed through the skin(JP-A-H1-85912). This system, however, leads to lowered compliance of the patient side because it needs the work of the destroying or bursting the user has to do upon application, and moreover has the defect that the manufacturing method is complicated. Further, the system poses the problem in the case of a patch preparation in which the medicine is contained in the layer of an adhesive, in that it lacks long-term preservability and introduces the lowering of the medicine content or eventually reduced therapeutic effect because the medicine gradually decomposes or deteriorates if the medicine is an unstable compound in the layer of an adhesive.
DISCLOSURE OF THE INVENTION
The object of the present invention is to provide a percutaneous absorption preparation which is simple in its use and manufacturing method, and which, even when the medicine is an unstable compound in the layer of an adhesive, makes the medicine preservative stably by restraining its decomposition and deterioration during preservation and which allows the medicine to move to the layer of adhesive and the skin and to be absorbed through the skin at the time of application of the preparation.
The inventors studied earnestly to solve the above problem and found as a result that the problem concerned was solved by the percutaneous absorption preparation which comprised a supporting body, a medicine storage layer, a permeation controlling film, a layer of an adhesive and a release liner and which was featured in that the above permeation controlling film was plasticized by moisture volatilized from the skin upon application of that preparation, thus achieving the present invention.
Namely, the present invention includes the following inventions.
(1) A percutaneous absorption preparation comprising a supporting body, a medicine storage layer, a permeation controlling film, a layer of an adhesive and a release liner, which is characterized in that the permeation controlling film is plasticized by moisture volatilized from the skin at the time of application of the preparation.
(2) A percutaneous absorption preparation according to the above (1), wherein the permeation controlling film is a water-soluble polymer.
(3) A percutaneous absorption preparation according to the above (2), wherein the water-soluble polymer is poly(vinyl alcohol).
(4) A percutaneous absorption preparation according to the above (1), wherein the medicine storage layer is formed by a medicine, or a medicine and a vehicle.
(5) A percutaneous absorption preparation according to the above (4), wherein the medicine is water-soluble.
(6) A percutaneous absorption preparation according the above (4), wherein the vehicle is a water-disintegrative substance.
(7) A percutaneous absorption preparation according to the above (1), wherein the supporting body has a water-vapor permeability of 100 g/m
2
or less at the condition of 40° C. and 24 hours.
(8) A percutaneous absorption preparation according to the above (1), wherein the adhesive has a water-vapor permeability of 100 g/m
2
or more at the condition of 40° C. and 24 hours.
(9) A percutaneous absorption preparation according to the above (1), wherein the therapeutic medicine is nicorandil, dopamine hydrochloride or eperisone hydrochloride.
The present invention is explained in detail in the following.
The percutaneous absorption preparation of the present invention is one which comprises a supporting body, a medicine storage layer, a permeation controlling film, a layer of an adhesive and a release liner and which is characterized in that the above-mentioned permeation controlling film is plasticized by moisture evaporating from the skin at the time of application of the preparation.
The word “plasticize” means “to make a substance prone to cause plastic deformation or plastic flow by an external force”, and in the case of the invention it means that the permeation controlling film gives rise to plastic flow because of its absorbing moisture and the medicine activated by moisture permeates, dissolves, disperses or diffuses into the permeation controlling film.
In the percutaneous absorption preparation of the present invention, it is necessary that the permeation controlling film is located between the medicine storage layer and the layer of adhesive and plasticized by moisture volatilized from the skin upon application of the preparation. Thus, the medicine, or the medicine and vehicle permeates, dissolves, disperses or diffuses into the permeation controlling film and moves to the layer of adhesive, and the medicine is absorbed through the skin. As the permeation controlling film any component may be used without limitation as long as it is plasticized by moisture evaporating from the skin and allows the permeation of the medicine when the preparation is applied. As such permeation controlling films there are enumerated water-soluble polymers, preferably synthetic polymers such as poly(vinyl alcohol) and poly(vinylpyrrolidone), polysaccharides such as soluble starch, dextrin, cellulose, methylcellulose and carboxymethylcellulose, natural polymers such as corn starch, sodium alginate, gum arabic, gelatin and pullulan, and inorganic polymers such as sodium polyphosphate and water glass. Most preferred is poly(vinyl alcohol).
In the percutaneous absorption preparation of the present invention, the medicine storage layer is formed by a medicine, or a medicine and a vehicle (excipient).
As the vehicle preferably enumerated are water-disintegrative substances, though there is no limitation as long as it is ones generally used. Here, “water-disintegrative substance” indicates “a substance which functions as a vehicle at the time of preparing the medicine storage layer and as a disintegrative agent in the presence of moisture at the time of applying the preparation.” Such water-disintegrative substances include, for example, saccharides such as glucose, lactose, sucrose, starch, soluble starch and methylcellulose, polyethyleneglycols and polysolbates.
As the therapeutic medicine used for the medicine storage layer, any may be employed without limitation as long as it is absorbed percutaneously. Preferable are amine type therapeutic medicines such as nicorandil, dopamine hydrochloride and eperisone hydrochloride.
Further, as the therapeutic medicine there are enumerated non-steroidal anti-inflammatory drugs, steroid type anti-inflammatory drugs, antiarrhythmic drugs, antitumor agents, hypnotics, psychotropic drugs, local anesthetic drugs, cardiotonic drugs, antibiotics, antituberculosis drugs, analgesic agents, muscular relaxants, anti-asthma drugs, anti-cholinergic agents, vasodilators, antihypertensive agents, antihistamines, cholinergic agents and angiotensin invertase inhibitors.
It is needed that the therapeutic medicine used in the percutaneous absorption preparation of the present invention permeates, dissolves, disperses or diffuses into the permeation controlling film that has been plasticized by moisture volatilized from the skin.
The medicine storage layer may incorporate, if necessary, additives such as kaolin, talc, bentonite, titanium oxide, calcium bi
Nakahara Kaname
Seki Toshinobu
Lintec Corporation
Oblon & Spivak, McClelland, Maier & Neustadt P.C.
Page Thurman K.
Sheikh Humera N.
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