Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1992-07-31
1995-02-07
Henley, III, Raymond J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
514458, 4241951, 424450, A61K 31665, A61K 31355, A61K 3722, A61K 3578
Patent
active
053875796
DESCRIPTION:
BRIEF SUMMARY
The present invention relates in general terms to the use of an .alpha.-tocopherol phosphate, or an ester thereof, or a salt of these compounds, for preparing pharmaceutical, cosmetic or dermatological compositions with antiallergic or antiinflammatory activity or for the prevention or treatment of the harmful effects of free radicals, and to pharmaceutical, cosmetic or dermatological compositions with antiallergic or anti-inflammatory activity or for the prevention or treatment of the harmful effects of free radicals, in which said compound is incorporated.
It is known that vitamin E has the common name of .alpha.-tocopherol in particular (see Merck Index, 10th edition, reference 9832, page 1437).
.alpha.-Tocopherol occurs in the natural state in numerous plants, usually with other compounds such as .beta.-tocopherol and .gamma.-tocopherol.
It is also known that .alpha.-tocopherol exists in both the dl and d forms.
.alpha.-Tocopherol is essentially used for controlling vitamin E deficiencies or as a nutritional factor, especially for controlling muscle degeneration.
It is also used as an antioxidant, but at very specific doses.
.alpha.-Tocopherol esters have also been described, in particular the succinate, the nicotinate or the acetate (Merck Index, 10th edition, references 9832, 9833, page 1437). The synthesis of .alpha.-tocopherol acetate is also described in U.S. Pat. No. 2,723,278 and that of other esters is described in the document J. Amer. Chem. Soc. (1943) 65, 918-924.
dl-.alpha.-Tocopherol phosphate is also known (see P. KARRER et al., Helv. Chim. Acta (1940) 23, 1137-8), as is its action on muscle metabolism (see J. Biol. Chem. 1942, 146, pages 309-321). Another document describes the biological role as an antioxidant on brain tissue (Biol. Antioxidants Trans., 1st Conf., 1946, pages 61-62). An anticoagulant action through an action on the polymerization of fibrin has also been described (Can. J. Biochem. and Physiol. 1959, 37, pages 501-505). An antimicrobial action in vitro on B. subtilis and S. aureus has also been described (Naturwissenschaften 1960, 47, page 17).
In another connection, German patent application A-3 416 209 describes the use of creams containing vitamin E for the treatment and prevention of inflammatory processes. By contrast, Berkenkopf and Lutsky have described that the injection of vitamin E into rats causes a chronic localized inflammation (Agents Actions 1979, 9, (4), 350-357).
Thus the action of vitamin E on inflammation is controversial.
It has now been discovered, totally surprisingly and unexpectedly, that .alpha.-tocopherol phosphate, especially in its dl or d form, or an ester thereof, of the general formula ##STR3## in which: R.sub.1 is a hydrogen atom, an alkyl radical having from 1 to 4 carbon atoms, such as the methyl or ethyl radical in particular, or an .alpha.-tocopheryl radical; and atoms, such as a methyl or ethyl radical in particular, or R.sub.2 O is an oxyethylene chain of the formula ##STR4## in which R.sub.3 and R.sub.4 independently are a hydrogen atom or a methyl radical and n is an integer greater than or equal to 1, dermatological or cosmetic composition for the prevention or treatment of allergic manifestations such as skin allergy or bronchial asthma, or inflammatory manifestations, or else for the prevention or treatment of the harmful effects of free radicals.
Thus the object of the present invention is to solve the new technical problem which consists in providing an active substance having a good antiallergic activity, especially for the prevention or treatment of skin allergy or bronchial asthma, or a good antiinflammatory activity, or else a preventive or curative activity against the harmful effects of free radicals, in particular by topical or general administration, thereby constituting a valuable active ingredient for preparing cosmetic, dermatological or pharmaceutical compositions.
The present invention solves this new technical problem satisfactorily with a particularly simple solution which can be used on the industrial scale.
Th
REFERENCES:
Chem. Abstracts 107(10):83908, Truia et al. Jul. 1986.
Bonte Frederic
Marechal Christian
Meybeck Alain
Henley III Raymond J.
LVMH Recherche
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