Nitto-denko Corporation

Toa Eiyo Ltd.

Shin-etsu Chemical Co., Ltd.

Shuichiro Yuasa

Katsuhiro Okada

Yoshihiro Iwao

Kunihiro Minami

Katsuyuki Ookubo

Ikuo Fukui

Kensuke Matsuoka

Yuichi Nishiyama

Yuichi Ito

Mutsunori Tanji

Tadashi Matsui

The present invention is an enteric coated granule having controlled dissolution in water even at a small coating amount; and a preparation method thereof. More specifically, provided are an enteric coated granule comprising a raw granule or a granule comprising a raw granule and at least one layer covering the raw granule, a first enteric layer covering the raw granule or the granule, and a second enteric layer formed over the first enteric layer, wherein the first and the second enteric layers comprise a first and a second hydroxypropylmethyl cellulose acetate succinates (HPMCASs) different in solubility pH, respectively, and the solubility pH value of the second HPMCAS of the second enteric layer is lower than that of the first enteric layer; and a preparation method comprising steps of covering a raw granule or a granule comprising a raw granule and at least one layer covering the raw granule with an enteric coating agent comprising a first HPMCAS to form a first enteric layer; and forming, over the first enteric layer, a second coating layer by using a second enteric coating agent comprising a second HPMCAS having a lower solubility pH value than that of the first HPMCAS.

Enteric coated granule and method for preparing the same

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.

Growing community of inventors

Fukushima, Japan

Shuichiro Yuasa