Toa Eiyo Ltd.

Nitto-denko Corporation

Kunihiro Minami

Katsuhiro Okada

Yoshihiro Iwao

Shuichiro Yuasa

Katsuyuki Ookubo

Tetsuya Nakamura

Kensuke Matsuoka

Tomoya Tanaka

Jun Ishikura

Kazuhiro Aoyagi

Naoko Urushihara

Yu Tachikawa

Satoshi Ameyama

Akira Yokouchi

Takayuki Furuishi

Yoshitaka Inoue

Takayuki Minowa

Miho Komine

Kunihiko Kimura

Eriko Abe

Naohiro Nishida

An adhesive preparation containing bisoprolol includes a backing and a pressure-sensitive adhesive layer formed on one side of the backing. The pressure-sensitive adhesive layer contains a polymer prepared through copolymerization of monomer components including a hydroxyl group-containing monomer and an alkyl (meth)acrylate monomer (component (A)), a polymer prepared through copolymerization of monomer components including a methyl methacrylate monomer and a butyl methacrylate monomer (component (B)), and bisoprolol (component (C)).

Adhesive preparation containing bisoprolol

An adhesive pharmaceutical preparation which has a less irritation to the skin surface, keeps excellent stability of bisoprolol in the preparation, and allows continuous administration of a pharmacologically effective amount of bisoprolol into the living body, is provided. The adhesive preparationcomprises a support, an adhesive layerlaminated on one surface of the support. The adhesive layeris characterized by containing bisoprolol, polyisobutylene, tackifier, and an organic liquid ingredient compatible to polyisobutylene and tackifier. Thus, an adhesive pharmaceutical preparation which has a good adhesiveness with less irritation to the skin and which gives almost no pain at peel-off or removal from the skin surface with leaving almost no paste, can be provided. In addition, bisoprolol is very stably maintained in the preparation and a pharmacologically effective amount of bisoprolol can be administered continuously into the living body through the skin surface.

Adhesive pharmaceutical preparation containing bisoprolol

The present invention relates to a percutaneous administration device of bisoprolol, which includes a backing; and a pressure-sensitive adhesive layer containing bisoprolol, which is laminated on one surface of the backing, wherein the maximum value of a release rate of bisoprolol during a period of from immediately after the application on skin until a lapse of 24 hours is 30 &#x3bc;g/cm/hr or less; and wherein the release rate of bisoprolol at the time of a lapse of 24 hours after the application on skin is 10 &#x3bc;g/cm/hr or less. The percutaneous administration device of the present invention is reduced in the skin irritation during the application, especially at the time of peeling, and is capable of persistently administrating a therapeutically or preventively effective amount of bisoprolol into a living body.

Percutaneous administration device of bisoprolol

In the adhesive pharmaceutical preparation of the invention containing bisoprolol, a pressure-sensitive adhesive layer is laminated on one side of the backing. The pressure-sensitive adhesive layer contains a branched monoalcohol having from 12 to 28 carbon atoms, a free base of bisoprolol and a polyisobutylene pressure-sensitive adhesive. Accordingly, compatibility of the polyisobutylene pressure-sensitive adhesive with the free base of bisoprolol can be specifically increased. As a result, not only it becomes possible to increase blending amount of the free base of bisoprolol but also bleed of the free base of bisoprolol from the pressure-sensitive adhesive layer can be suppressed and, what is more, the pressure-sensitive adhesion characteristics sufficient from the practical point of view can be obtained.

A proline ester represented by the following formula (I): wherein Rrepresents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.

Proline ester and preparation containing the same for percutaneous administration

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Fukushima, Japan

Kunihiro Minami