Percutaneously absorbable patch

Details Percutaneously absorbable patch Percutaneously absorbable patch

1997-04-28

1998-10-13

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

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

424448, A61F 1302, A61L 1516

Patent

active

058208780

DESCRIPTION:

BRIEF SUMMARY
This application is a 35USC371 of PCT/JP95/02336 filed Nov. 15, 1995.


TECHNICAL FIELD

This invention relates to a percutaneously absorbable preparation-containing patch suitable for persistently releasing estrogen and luteal hormone as medicinal ingredients from the preparation.


BACKGROUND ART

Estradiol contained in estrogen is secreted from the ovary of a woman during her reproducible period of time. Thus, women who are at the menopause or thereabouts become lacking in estradiol whereupon they suffer from their menopausal disorder, irregular menstruation or the like. Remedies for these symptoms are now taken by the use of orally administrable preparations, but these preparations are rapidly metabolized by digestive canals such as stomachs and intestines and also by livers to be made inactive. Thus, in order to obtain sufficient medicinal efficacy, a large dose of estradiol must be administered. The use of such a high dose is very likely to cause adverse side effects and the like.
Accordingly, the use of estradiol in combination with luteal hormone, which, through percutaneous administration, can reduce the metabolism of estradiol and permits the estradiol to reach blood and, at the same time, inhibits the side effects of the estradiol per se, has been studied in the art.
For example, Japanese Pat. Appln. Laid-Open Gazette No. 342532/92 discloses a percutaneously absorbable preparation which comprises estradiol and luteal hormones as active ingredients and a tackifier composed mainly of an acrylic tackifier consisting of 2-ethylhexyl acrylate and N-vinyl-2-pyrrolidone. The acrylic tackifier, however, has poor capability of releasing drugs and has strong irritation to the skin, thereby rendering said preparation unsuitable for continuous administration for a long period of time. Japanese Patent Gazette No. 51623/94 discloses a method wherein estradiol and norethisterone acetate as active ingredients are dissolved in a gel comprising hydroxypropyl cellulose and ethanol, this is then formed to a reservoir type, and the release of the active ingredients is regulated with the aid of a permeant regulating membrane. Ethanol, however, has strong irritation to the skin and causes side effects such as rubefaction at preparation-applied sites very frequently.
The percutaneously absorbable patches containing a preparation under various studies as mentioned above are low in biological utility since the active ingredients contained therein can be used only to a limited extent. In addition, the tackifier per se or the addition of absorption accelerators such as ethanol will raise a problem of skin irritation since the preparation is attempted to be percutaneously administered.


SUMMARY OF THE INVENTION

In view of the above disadvantages, the inventors of this invention have made intensive studies with a view to providing percutaneously absorbable patch containing a preparation, which has
Thus, the percutaneously absorbable preparation-containing patch of this invention comprises: (1) a base comprising as essential ingredients a (A-B) n-A based elastomer (elastic polymer) (wherein A is substantially a monovinyl-substituted aromatic compound polymer block, B is substantially a conjugated diolefin copolymer block and n is an integer of 3-7), crotamiton and a softening agent; and (2) at least two hormones as active ingredients.
According to this invention, at least two hormones are contained as the active ingredients. Estrogen and luteal hormone are usually used as the two active ingredients.
Examples of the estrogen are estradiol, estrone, estriol, equilin, equilenin and derivatives thereof. Among them, estradiol is usually used in the percutaneously absorbable preparation contained in the patch according to this invention.
The luteal hormone is suitably selected from the group consisting of progesterone, hydroxyprogesterone caproate, medroxyprogesterone acetate, dydrogesterone, chlormadinone acetate, ethisterone, dimethisterone, norethisterone, norethisterone acetate, norethisterone enanthate, ethynodial acetate, m

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