Transdermal preparation

Abstract

Provided is a transdermal preparation, which is capable of long-term (1-day to 7-day) release of a basic drug from a preparation, continuously and at a consistent concentration; shows little reduction over time in the drug content, even if multiple drugs are contained in the preparation; and is produced by a simple process. The transdermal preparation comprises a substrate, and an adhesive layer containing a basic drug and a water-soluble polymer.

Description

[0001]This patent application is a U.S. National Stage Application of International Application No. PCT / JP2010 / 057659, filed Apr. 30, 2010, which claims the benefit of priority from Japanese Application No. 2009-112234, filed May 1, 2009, teachings of each of which are herein incorporated by reference in their entirety.TECHNICAL FIELD[0002]The present invention relates to a transdermal preparation that continuously delivers a certain amount of a drug through the skin.BACKGROUND ART[0003]To obtain drug effects from a drug by its administration, an oral administration method is generally used; however, transdermal administration methods have many advantages over oral administration methods. For example, in an oral administration method, the drug absorbed in the bowel is, before it exhibits a drug effect in a desired site, first metabolized in the liver and most of its quantity is decomposed; whereas in a transdermal administration method, since the absorbed drug does not first pass th...

AI Technical Summary

Benefits of technology

[0036]Regarding the transdermal preparation of the present invention, its production process is simple, and the drug can be transdermally absorbed at a stable skin permeation rate continuously for a long period of time, and time-course stability of the drug is good, and its adhesion to the skin is good, with only a little irritation to the skin; accordingly, the transdermal preparation of the present invention is extremely effective to the treatment of a wide range of disorders.

Problems solved by technology

However, because many basic drugs are low soluble to rubber adhesives and silicone adhesives, it is very difficult to contain a basic drug with 10 mass % or more in these adhesives while maintaining properties of the adhesives.

Meanwhile, to produce a transdermal administration preparation comprising a basic drug with the high concentration of 10 mass % or more, use of an acrylic adhesive having high polarity is advantageous in terms of solubility to drugs; however, many basic drugs react with acrylic acid alky ester or acrylic acid, i.e., a constitutional monomer of acrylic adhesives, possibly leading to a problem of a decrease in the drug content, etc.

However, when bisoprolol is orally administered, it may possibly induce symptoms such as bradycardia, dizziness, and malaise; from the viewpoint of stability of blood concentration over long period of time and sustainability of effects, development of transdermal administration preparations such as adhesive patches has been desired, rather than oral administration.

When SSRI such as fluvoxamine is orally administered to a patient, side effects such as nausea, diarrhea, and gastrointestinal tract disturbance are concerned, and defect of decreased compliance occurs such as withdrawal of taking the drug.

However, since an acrylic adhesive is used for the drug reservoir layer, the drug content tends to decrease during long period of storage.

However, in this literature, it is not that a basic drug is contained in a high concentration by means of comprising water-soluble polymer in the adhesive patch, and a means for achieving this is not provided as well.

However, this literature neither enables to contain a basic drug in a high concentration, nor provides a means for achieving this.