Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1997-03-11
1999-06-22
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514549, A61K 3120, A61K 3122
Patent
active
059143479
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the field of pharmacy, more particularly to that of therapeutic chemistry and to that of dermato-cosmetology.
More particularly, it relates to a process for the stabilisation of polyunsaturated fatty acids with a view to reliable and prolonged therapeutic use.
Interest in polyunsaturated acids, especially .alpha.- or .gamma.-linolenic acid (vitamin F) has been increasing for several years because of their special role in various biological syntheses. For this reason, it has been possible to regard polyunsaturated fatty acids of the 18:3 series and particularly of the 20:3 series as key precursors and intermediates in the formation of prostaglandins PGE1 following a series of enzymatic reactions due to specific desaturases and to elongases.
Interest in unsaturated fatty acids in dermatology and cosmetology has also been increasing because of their regenerative and anti-ageing properties for the epidermis. In this respect, the properties of polyunsaturated fatty acids depend not on a possible conversion to prostaglandins or prostacyclins, but on a direct effect.
The use of polyunsaturated fatty acids in therapeutics derives from their ability to be converted to prostaglandins, and more particularly PGE.sub.1 which have an important mediating function in the regulation of arterial pressure, in the motor function, in promoting the contraction of smooth muscle and in preventing gastric ulcers.
The hopes of using these acids have not been realised, on the one hand because of their poor degree of assimilation but on the other hand, and above all, because polyunsaturated fatty acids are oxidised readily and rapidly under the action of light, peroxides and, in particular, atmospheric oxygen, leading to the formation of resins.
Consequently, polyunsaturated fatty acids such as linolenic acids, stearidonic acid, eicosapentaenoic acid or dihomo-.gamma.-linolenic acid or the synthetic analogues thereof readily undergo oxidation, hydroxylation or peroxidation, leading to metabolites with little or no activity which the body rejects or excretes. This is particularly the case with dihomo-.gamma.-linolenic acid (cis 8, cis 11, cis 14-eicosatrienoic acid), the synthetic analogues thereof and with arachidonic acid (cis 5, cis 8, cis 11, cis 14-eicosatetraenoic acid).
In view of the therapeutic use, it appeared necessary therefore to have a means of preventing the oxidation of said polyunsaturated fatty acids or their esters if it is desired to keep them chemically intact and above all if it is considered important to retain the possibility of their being metabolised in the body to prostaglandins and/or prostacyclins. Indeed, the hydroxylated or oxidised decomposition products are inactive because they are not resorbed in the digestive tract or because they can no longer be converted by enzymatic systems to higher fatty acid homologues.
The aim, therefore, was to find a method of stabilising polyunsaturated fatty acids or their esters which enables them to remain stable without auto-oxidation and thus to act as a prodrug for prostaglandins. It is known that .gamma.-linolenic acid or .alpha.-linolenic acid are converted rapidly under the action of specific desaturases and of elongases to dihomo-.gamma.-linolenic acid, stearidonic acid and then to prostaglandins PGE, the beneficial effects of which on gastric cytoprotection are well-known. It is important to keep this enzymatic transformation fully intact.
When applied topically, polyunsaturated fatty acids also play an important part in maintaining or restoring the youth of the integument; numerous patents have shown the advantage of cosmetic, dermatological and nutritional preparations of polyunsaturated fatty acids.
In particular, attention is drawn to numerous patents which are interesting in that they show the topical use of polyunsaturated fatty acids, more specifically: a patent to INDENA dated Jul. 27, 1987 entitled "Polyunsaturated acids having vasokinetic action and pharmaceutical and cosmetic formulations containing them". The author
REFERENCES:
patent: 2827452 (1958-03-01), Schlenk et al.
patent: 3450821 (1969-06-01), Carstensen et al.
patent: 4897421 (1990-01-01), Braquet
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