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Title:
SUSTAINED RELEASE EXTERNAL PREPARATION FOR SKIN CONTAINING TOCOPHEROL
Document Type and Number:
Japanese Patent JPH1025244
Kind Code:
A
Abstract:

To obtain the subject external preparation which contains a specific tocopherol glycoside as an active ingredient and keeps tocopherol stably in the preparation and can gradually reveal tocopherol by starting the release of the tocopherol glycoside, when it is applied to skin surface.

A tocopherol glycoside of the formula (R1 is a residue of a saccharide selected from the group consisting of glucose, xylose and maltose; R2 and R3 are each H, methyl) is used as an active ingredient. The tocopherol glycoside of the formula is prepared, for example, by reaction of tocopherol with a desired peracetylated saccharide in a suitable solvent in the presence of a Lewis acid catalyst, for example, aluminum trichloride or boron trifluoride to form an intermediate having R1 of the residue of the acetylated saccharide, refluxing the product in anhydrous ethanol in the presence of sodium methoxide with heat, followed by deacetylation with an acid-type ion-exchange resin. The compound of the formula is, for example, dl-α-tocopherylglucoside or the like and the concentration of this glycoside is preferably about 0.01-3wt.% in the preparation.


Inventors:
IWAMOTO MINORU
ITO MASAMICHI
Application Number:
JP20131496A
Publication Date:
January 27, 1998
Filing Date:
July 11, 1996
Export Citation:
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Assignee:
HASEGAWA T CO LTD
International Classes:
C07H17/075; A61K8/00; A61K8/34; A61K8/60; A61K9/06; A61K31/70; A61K31/7042; A61K31/7048; A61P3/02; A61P17/00; A61Q19/00; C07D311/72; (IPC1-7): A61K31/70; A61K7/00; A61K7/48; A61K9/06; A61K31/70
Attorney, Agent or Firm:
Masaaki Kobayashi