Estradiol percutaneous administration preparations

Details Estradiol percutaneous administration preparations Estradiol percutaneous administration preparations

1992-03-09

1993-09-28

Schenkman, Leonard

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

424449, 514947, A61K 3156

Patent

active

052486761

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to an estradiol percutaneous administration preparation suitable for durably releasing estradiol therefrom.


PRIOR ART

Estradiol is estrogen (follicle hormone) 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 symtoms are now made by the use of orally administrable preparations, but these preparations are rapidly metabolized by digestive canals such as stomachs and intestines, and livers so that they become 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 reactions and the like.
Therefore, some publications indicate that the percutaneous administration of preparations without passage through digestive canals and the liver has been studied. They include, for example, Japanese Pat. Appln. Laid-Open Gazette No. Sho 57-154122 or No. 154122/82 which discloses a method for controlling the release of estradiol dissolved in a hydroxypropylcellulose-ethanol gel through an ethylene-vinyl acetate membrane, Japanese Pat. Appln. Laid-Open Gazette No. Sho 60-152413 or No. 152413/85 which discloses only a menthol-containing percutaneous absorption preparation as a percutaneous absorption accelerator but is silent about pasting agents, Japanese Pat. Appln. Laid-Open No. Sho 61-17513 or No. 17513/86 which discloses a medicinal composition using therein a medicine permeation accelerator obtained by mixing propylene glycol with glycerine in a specified ratio, Japanese Pat. Appln. Laid-Open Gazette No. Sho 61-155321 or No. 155321/86 discloses a tackifier base containing as the principal ingredient a polymer capable of swelling in water, the polymer being illustrated by, as a tackifier base, tacky resin materials (polyterpene resins, hydrocarbon resins, etc.), natural or synthetic rubber (polyisobutylene, styrene-butylene polymers, styrene-isoprene polymers, styrene-ethylene-butylene polymers, 1,4-polyisoprene, etc.), galactmonnane, etc., and Japanese Pat. Appln. Laid-Open Gazette No. Sho 63-233916 or 233916/88 which discloses a pasting agent relative to a device composed of 7-layer laminated body.
The estradiol percutaneous administration preparations under various studies as mentioned above need specified processes in the production of the preparations because of their complicated structure and the like and therefore need an expensive apparatus to produce them. Further, the preparations are low in biological utility since the active materials contained therein can be used only to a limited extent. In addition, the addition of absorption accelerators such as ethanol will raise a problem as to skin stimulation from the standpoint of percutaneous administration.
In view of the above disadvantages, the present inventors made intensive studies in attempts to provide estradiol percutaneous administration preparations which have a simple structure, improved biological utility and lower skin stimulation and, as the result of their studies, they accomplished the present invention.


Disclosure of the Present Invention

The estradiol percutaneous administration preparation of the present invention comprises as the base:
1) (A-B) nX or (A-B) n-A type elastomer (elastic polymer) wherein A is substantially a monovinyl-substituted aromatic compound polymer block, B is substantially a conjugated diolefin copolymer block, n is an integer of 3-7, and X is a residue derived from a polyfunctional compound and combined with n of polymer chain (A-B),
2) crotamiton and
3) a super absorbent polymer and further comprises estradiol as the medicinal ingredient.
Estradiol used in the present invention is generally called estra-1. 3. 5 (10) trienne-3.17.beta.-diol and is represented by the following structural formula ##STR1##
The percutaneous administration preparations of the

REFERENCES:
patent: 4994267 (1991-02-01), Sablotsky
Serveur Eqoque & File Japs, & JP-A-60 188-314 (Yamanouchi Seitaku K.K.) Sep. 25, 1985--Whole Abstract.
STN File Server, File CA & Chemical Abstracts, vol. 113, No. 8, abstract No. 65348r. Columbus Ohio U.S.; and JP-A-01 297,069 (Hisamitsu Pharmaceutical Co., Inc.) Nov. 30, 1989-whole abstract.

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