External escinol preparation for skin

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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Details

514 33, 514561, 424 62, A01N 4304, A61K 3170

Patent

active

057286833

DESCRIPTION:

BRIEF SUMMARY
This is a 371 of PCT/JP95/01360 filed Jul. 7, 1995.
The present invention relates to an external preparation for skin and, more particularly, to an external preparation for skin which is excellent in whitening effect and has good usability and safety.
Aging phenomenon in skin which is exemplified by lines at corners of eyes and deposition of pigment such as spots and freckles appears earlier than that in other tissues and organs. It is often observed at an age as early as middle twenties. This is supposed to be because that the skin is at the outermost layer of an organism where it is likely to receive external stimulation (i.e., stress) such as ultraviolet rays, oxygen, and chemical substances.
The deposition of melanin pigment on the skin such as spots or freckles due to ultraviolet rays and stress occurs when pigment cells, which are melanin-producing cells, grow or the melanin-producing function within the pigment cell is accelerated. Recent studies have been elucidating that spots and freckles are generated when factors for activating the pigment cells within the skin increase in this manner due to the ultraviolet rays and stress.
Conventionally, in order to prevent these obstacles in the skin and to attain whitening effect, ascorbic acid and its derivatives have been widely used.
However, it is difficult for conventionally-used ascorbic acid and its derivatives to sufficiently exhibit the effect on preventing the deposition of pigment.
On the other hand, escinol is a kind of triterpenoid saponin formed when escin (i.e., a mixture of a plurality of kinds of saponin) in an extract of seeds of Asculus hippocastanum L is alkali-decomposed so as to eliminate its acyl group. It does not exist in the extract of seeds of Asculus hippocastanum L and in escin.
Since the extract of seeds of Asculus hippocastanum L has an anti-inflammatory effect, it has been known to be compounded in cosmetic preparations in order to prevent the skin from flushing (Japanese Unexamined Patent Publication Sho No. 53-9328, Japanese Unexamined Patent Publication Sho No. 62-81306, and Japanese Unexamined Patent Publication Hei No. 2-117619). Also, it has been clarified that escin has an anti-inflammatory effect as an effective ingredient in the extract of seeds of Asculus hippocastanum L (Oyo Yakuri 9:883, 1975).
Further, the inventors have elucidated that escin has an effect on resistance to the deposition of pigment, i.e., whitening effect (Japanese Patent Application Hei No. 5-246161). However, it has not yet been known at all that escinol has a whitening effect.
In view of the above-mentioned problem of the prior art, the object of the present invention is to provide an external preparation for skin which is excellent in whitening effect, by which the deposition of pigment is suppressed directly and effectively, and has good usability and safety.
As the result of diligent studies of the inventors for attaining the above-mentioned object, it has been found that escinol and its salts have an excellent whitening effect and are excellent in usability and safety. Accordingly, the present invention has been achieved.
Namely, the present invention provides an external preparation for skin comprising one or more than two members selected from the group consisting of escinol and its salts.
In the following, the constitution of the present invention will be explained in detail.
Escinol and its salts in the present invention have an effect on suppressing the production and action of factors for activating pigment cells in the skin. As a result, production of melanin in the pigment cells and abnormal growth of the pigment cells are suppressed.
Escinol and its salts, which are effective ingredients in the external preparation for skin in accordance with the present invention, are a compound represented by the following constitutional formula (1) (escinol) and its salts and have been known to have a cytotoxicity much lower than that of escin (Folia Histchemica et Cytchemica 16:69, 1978). ##STR2## (wherein R.sup.1 is hydrogen atom or hydroxyl

REFERENCES:
patent: 5541220 (1996-07-01), Ismail
patent: 5580549 (1996-12-01), Fakuda et al.
Ogura, Suzuki, Tamada & Fujimoto Studies on the Anti-Inflammatory Action of Horse-Chestnut Saponin (1975).
Yoshikawa et al. Escins-la,lb,lla,llb, and IIIa . . . Jun. 1994.
Mitsubishi Rayon Co. Ltd. Back Protection Screen, abstract Oct. 1987.
Shiseido Co.Ltd. External Agent for Skin, abstract Sep. 1986.
Shiseido Co.Ltd. Dyestuff Deposition Inhibitor, abstract Mar. 1995.
CA 114:181954, Omelkova et al. 1990.

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