Percutaneously absorbable preparation containing cohesive streng

Details Percutaneously absorbable preparation containing cohesive streng Percutaneously absorbable preparation containing cohesive streng

1997-03-12

1998-09-22

Brouillette, D. Gabrielle

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

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

424449, A61F 1302

Patent

active

058111174

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP95/01442, filed Jul. 20, 1995.


TECHNICAL FIELD

The present invention relates to a percutaneous pharmaceutical preparation with improved percutaneous absorbability and a low skin irritation.


BACKGROUND ART

Norethisterone and estradiol, inclusive of their esters, are known as female hormones. Administration of estradiol or an ester thereof is a well-established, effective treatment for the control of characteristic mental symptoms in climacteric women and prevention of osteoporosis due to loss of bone minerals. As to norethisterone or its ester, its administration is essential to the prevention of side effects of estrogens such as estradiol.
For the avoidance of adverse effects such as hepatic disorder and in view of the ease to maintain a constant blood concentration, it is preferable that such female hormones be administered percutaneously. As dosage forms suited for this purpose, U.S. Pat. No. 4,788,062 discloses a percutaneous pharmaceutical preparation utilizing a fatty acid ester such as sucrose monolaurate, glycerol monooleate, or glycerol monolaurate as an absorption enhancer. Japanese Kokai Publication Hei-4-342531 describes a percutaneous pharmaceutical preparation containing at least one member of hydroxycarboxylic acids and N-acylsarcosines as an absorption enhancer and Japanese Kokai Publication Hei-2-102656 discloses a percutaneous pharmaceutical preparation containing an amide compound and a fatty acid ester as absorption enhancers. Furthermore, directed to drug compounds which are rather easily absorbed percutaneouly, e.g. nitroglycerin, Japanese Kokai Publication Hei-3-291217 proposes a technology in which a fatty acid ester is added in a substantial proportion to an acrylic adhesive not containing a polar functional group to realize a marked improvement in absorption enhancing effect and, to further enhance the cohesive strength of the adhesive layer, a hydrophilic silicic anhydride and a hydrophobic silicic anhydride are used in combination.
However, with respect to estradiol, norethisterone, and their esters, fatty acid esters in general do not provide sufficient absorption enhancing effect, while surfactants such as hydroxycarboxylic acids and N-acylsarcosines have potent percutaneous absorption enhancing effects for these steroid hormones but have high dermal irritation proportional to their contribution to enhancing effect. Moreover, when they are used in combination with a fatty acid ester, an absorption enhancing effect commensurate with the formulated amount is obtained but the cohesive strength of the adhesive layer is decreased to cause the problem of adhesive-transfer to the skin. Moreover, in the case of an acrylic adhesive like that described in Japanese Kokai Publication Hei-3-291217, there are such problems that the low solubility of said hormones makes it impossible to add a sufficient amount of the active substance and the consequent short duration of efficacy calls for several dosings a day. Thus, the preparations provided by the conventional technologies are poor in compliance partly because, in the absence of an absorption enhancer, a large patch size is required for sufficient absorption, thus causing a feeling of physical disorder on prolonged application, and partly because the duration of efficacy is short, while the preparations with dermal permeation improved by addition of absorption enhancer satisfy the need for permeation but have the drawbacks of skin irritation and adhesive-transfer to the skin on peeling off, thus being unsuited for long-term therapy.


SUMMARY OF THE INVENTION

In view of the above state of the art, the present invention has for its object to provide a percutaneous pharmaceutical preparation which offers a high percutaneous absorbability for norethisterone, estradiol, and their esters, with satisfactory application characteristics and a low skin irritation.
The present invention relates to a percutaneous pharmaceutical preparation prepared by laminating an adhesive layer comprising an adhesive and an

REFERENCES:
patent: 4880416 (1989-11-01), Horiuchi
patent: 5079008 (1992-01-01), Sinnreich
patent: 5128138 (1992-07-01), Blank
patent: 5260064 (1993-11-01), Nakagawa
patent: 5650165 (1997-07-01), Akemi

Affiliated with

Also associated with

Rating

Percutaneously absorbable preparation containing cohesive streng does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Percutaneously absorbable preparation containing cohesive streng, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Percutaneously absorbable preparation containing cohesive streng will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1620258