Percutaneous preparation

Details Percutaneous preparation Percutaneous preparation

1998-11-24

2000-06-20

Richter, Johann

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Web, sheet or filament bases; compositions of bandages; or...

424449, 544370, A61F 1302, A61K 970, C07D40304

Patent

active

060775289

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The present invention relates to a percutaneous preparation that can maintain 6-amino-5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl)benzimidazole or an acid addition salt thereof stably in the preparation and that enables continuous and percutaneous administration thereof to a living body.


BACKGROUND ART

Due to the superior serotonin.sub.3 receptor antagonistic action, 6-amino-5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl)benzimidazole and an acid addition salt thereof (hereinafter they are also referred to as benzimidazole compound) of the formula (1): ##STR1## are known to be useful compounds as antiemetic agents against emesis caused by cancer chemotherapy using cisplatin and the like (Japanese Patent Unexamined Publication No. 17449/1993). Also, it has been already known that a percutaneous preparation containing a benzimidazole compound as an active ingredient exhibits serotonin.sub.3 receptor antagonistic action upon percutaneous absorption of said benzimidazole compound (Japanese Patent Unexamined Publication No. 48258/1995).
However, a percutaneous preparation containing the above-mentioned benzimidazole compound as an active ingredient is unsatisfactory in the stability of the benzimidazole compound, which is the main drug, contained in the preparation.


DISCLOSURE OF THE INVENTION

It is therefore an object of the present invention to provide a percutaneous preparation superior in percutaneous absorption of benzimidazole compound and duration of efficacy, that exhibits an improved stability of the benzimidazole compound (which is as an active ingredient) in the preparation.
That is, the present invention provides the following. least one side of a substrate, said layer comprising an acrylic copolymer, a benzimidazole compound and 2-mercaptobenzimidazole. comprises the acrylic copolymer, a fatty acid ester miscible with said acrylic copolymer, a benzimidazole compound and 2-mercaptobenzimidazole. acrylic copolymer: fatty acid ester weight ratio of 1:0.1-1:1. acrylic copolymer: fatty acid ester weight ratio of 1:0.25-1:2, and said acrylic copolymer is crosslinked. crosslinked by at least one kind of a crosslinking agent selected from the group consisting of an alcholate and a metal chelate, both comprising titanium or aluminum, and a trifunctional isocyanate.
By forming a percutaneous preparation comprising an acrylic copolymer as a base material for a benzirmidazole compound, the benzimidazole compound is percutaneously absorbed to exhibit superior serotonin.sub.3 receptor antagonistic action that lasts for an extended period of time. In particular, a percutaneous preparation further comprising a fatty acid ester alleviates or disperses the stress that works on the skin surface when removing said preparation. As a result, adhesion to the skin and stimulation to the skin can be balanced well. Moreover, addition of 2-mercaptobenzimidazole to said preparation improves the stability of the benzimidazole compound, which is an active ingredient, in the preparation.
While the substrate to be used for the inventive percutaneous preparation is free of any particular limitation, a preferable substrate does not permit decrease of the contents of the benzimidazole compound, 2-mercaptobenzimidazole and fatty acid ester in the adhesive layer, which is caused by the release thereof from the rear surface through the substrate. Thus, a substrate made from a material impermeable to these ingredients is preferable.
Specifically, used is a single film or a laminate film of polyesters such as polyethylene terephthalate, polyamides such as nylon, polyolefins such as polyethylene and polypropylene, poly(vinyl chloride), thermoplastic poly(vinyl chloride), thermoplastic vinyl acetate-vinyl chloride copolymer, poly(vinylidene chloride), ethylene-vinyl acetate copolymer, cellulose acetate, ethyl cellulose, ethylene-ethyl acrylate copolymer, polytetrafluoroethylene, polyurethane, ionomer resin, metal foils such as aluminum foil, and the like.
The thickness of the substrate is such that the perc

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