Topical composition for promoting transdermal absorption of ther

Drug – bio-affecting and body treating compositions – Face or body powders for grooming – adorning – or absorbing

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Details

424 7802, 424 7803, A61K 7035

Patent

active

057595283

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to a composition for topical application. More particularly, the present invention relates to a composition for topical application capable of dissolving the corneal layer of the skin at the surface of the skin acting as a barrier to prevent the invasion of foreign matter from outside the body and capable of preventing the leakage of humor etc. from inside the body and which promotes the absorption of a medicine from the skin. The present invention relates to a composition for topical application suitable for releasing a bioactive agent through the protective outer layer of the skin where it is applied and to the underlying tissue or the systemic circulation. Here, the term bioactive agent means a "skin agent effective for the skin" or a "treatment agent effective for the organs where cure is needed". The term "skin agent effective for the skin" means a chemical substance which has a beneficial topical effect when applied to the skin and has beautifying properties (for example, through protection of the skin against external factors or through improvement of the external appearance) or therapeutic properties (for example, through alleviation of the severity of a skin disease).
The term "treatment agent effective for the organs where cure is needed" means an agent which enters the systemic circulation and has a therapeutic effect when administered through intravenous injection, intramuscular injection, oral administration, rectal or buccal routes, and other various routes.


BACKGROUND ART

As the methods of administration of a medicinal ingredient, oral administration, administration by injection subcutaneously, intramuscularly, and intravenously, administration to the mucous membrane in the rectum or mouth, etc. are used in the past. Among these, oral administration is most general. However, in the case of oral administration, the medicinal ingredient is absorbed in large quantities in a short time frame, and therefore, it is difficult to control the concentration in the blood. Further, the absorbed medicinal ingredient sometimes loses its efficacy due to metabolis in the liver at the time of its first circulation. Further, in the case of an irritative medicinal ingredient, its administration easily causes side effects such as damage to the stomach or intestines and has numerous other problems. In recent years, to alleviate these side effects and problems, external preparations designed for transdermal administration have been developed. However, even with these external preparations, sufficient transdermal absorption of the medicinal ingredient is often not obtained and it is difficult to say that the objective has been sufficiently achieved. That is, the surface of the skin is called stratum corneum epidermidis skin and has the biological functions of preventing the intrusion of foreign matter from outside the body and preventing the leakage of humor from inside the body, and therefore, there was the problem that a sufficient transdermal absorption could not be obtained simply by mixing a medicinal ingredient into a substrate used in the past for external preparations.
To improve these problems, in recent years various keratolytic agents for promotion of transdermal absorption comprising keratolytic agents have been proposed and have been mixed in substrates of external preparations as a matter of routine. As such agents for promotion of transdermal absorption, there are known for example, dimethyl sulfoxide, dimethylformamide, dimethylacetamide, methyldecyl sulfoxide, etc. These cannot be said to be sufficient in terms of the effect of promoting transdermal absorption, safety, or feeling of use. Contrary to this, Japanese Unexamined Patent Publication (Kokai) No. 58-15910 describes the combination of cineole and a medicine, while Japanese Unexamined Patent Publication (Kokai) No. 63-77825 describes the combination of cineole, a nonionic surfactant, water, and a medicine so as to improve the safety and skin permeation of the medicine. Hifuka Kiyo (Dermatolo

REFERENCES:
patent: 3933422 (1976-01-01), Saad
patent: 3961044 (1976-06-01), Kelly et al.
patent: 4213912 (1980-07-01), Varma
patent: 4866201 (1989-09-01), Motojima et al.

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