Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1996-09-26
1998-03-31
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514315, 514473, 514549, 514557, 514724, 514738, 514552, A61K 31045, A61K 3119, A61K 3122, A61K 3134
Patent
active
057339007
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to a percutaneous administration base composition (or percutaneously administrable base composition) which enhances a medicine in percutaneous absorbability and is a low irritative to the skin and also relates to a percutaneous administration medicinal composition in which a medicine is contained in said base composition.
BACKGROUND ART
Methods of administering a medicine (or drug) which have heretofore been known, include those of peroral, rectal, hypodermic and intravenous administrations, among which peroral administration has widely been adopted. However, peroral administration of a medicine is disadvantageous in that, for example, the medicine is subject to primary metabolism at the liver after the absorption thereof, and an unduly high concentration of the medicine is temporarily appreciated after the administration thereof. Further, it has often been reported that side effects such as gastroenteric tract troubles, nausea and lack of appetite are caused when a medicine is perorally administered.
Percutaneous administration of a medicine has recently been noted in attempts to avoid such disadvantages of peroral administration and to meet the requirements of safe and sustained absorption of the medicine. In view of the above, the development of medicines for external application has been positively promoted and the medicines so developed have already been on the market.
Such percutaneous administration preparations, however, are yet often insufficient in percutaneous absorption of the medicine and, therefore, it cannot be said in fact that the object to provide a desired preparation is fully attained. More particularly, since the normal skin originally has a barrier function to prevent foreign matters from permeating into the body, the base singly used as such in an ordinary percutaneous administration preparation will not let the medicine used therein be fully percutaneously absorbed. It is thus required that the permeability of the medicine through the homey layer of the skin be controlled to enhance the medicine in percutaneous absorbability.
To this end, it is generally tried that a so-called percutaneous absorption promoter is added to the base. The absorption promoters which have already been proposed, include a combination of dimethylacetoamide with ethyl alcohol, isopropyl alcohol, isopropyl palmitate or the like (U.S. Pat. No. 3,472,931); a combination of 2-pyrrolidone with a suitable oil or with an ester of a straight-chain fatty acid and an alcohol (U.S. Pat. No. 4,017,641); and a combination of a lower alcohol with one of an alcohol having 7-20 carbon atoms, an aliphatic hydrocarbon having 5-30 carbon atoms, an ester of an aliphatic carboxylic acid with an alcohol, a mono- or diether having 10-24 carbon atoms and a ketone having 11-15 carbon atoms, and also with water (Japanese Pat. Appln. Laid-Open Gazette No. Sho 61-249934).
It cannot be said yet, however, that the above conventional absorption promoters and absorption promoting compositions are sufficiently safe for the skin. Further, it is attempted to enhance a basic medicine in percutaneous permeability by having an organic acid contained in a preparation comprising the basic medicine and, however, such attempt does not exert sufficient remedial effects as yet. Furthermore, a low irritative absorption promoting composition is reported in Japanese Pat. Appln. Laid-Open Gazette No. Hei 2-115131; however, this composition is still appreciated to be irritative to the skin site where it is administered in case of subjects who are highly susceptible to an alcohol.
DISCLOSURE OF THE INVENTION
This invention has been made to solve the problems of the above-mentioned conventional techniques and has for its object to provide a percutaneous administration base composition which enhances a medicine in percutaneous absorbability when the medicine is contained in the base composition and is remarkably low in irritation to the skin where a medicinal composition is administered and also to provide an exce
Higo Naruhito
Komori Ken-ichi
Hisamitsu Pharmaceutical Co. Inc.
Spivack Phyllis G.
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