Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1994-04-20
1996-12-31
Geist, Gary
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
A61K 3120
Patent
active
055895085
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP92/02285, filed Oct. 2, 1992.
TECHNICAL FIELD
The invention concerns the use of an emulsion that contains one or more, polyunsaturated, long-chain omega-3 fatty acids and/or omega-6 fatty acids or their pharmaceutically tolerable esters or salts for, respectively, the intravenous administration for the treatment of skin diseases, or to prepare an intravenously administered medicament for treating skin diseases, particularly inflammatory skin diseases, as well as diseases of the dermatitis and eczema family, in particular of skin diseases of the dermatitis and eczema family.
Today, skin diseases represent a high percentage of diseases in humans and animals with, for example, psoriasis are among the most common skin diseases, from which approximately 1 to 2% of the population suffers.
STATE OF THE ART
The necessity of essential fatty acids for the structure and function of the skin is known. Using animal models, rats have who were given a diet free of these fatty acids have exhibited developmental impairments and skin alterations with reddening, dandruff, and hyperkeratoses in the region of the sebaceous glands. Other alterations included increased effluvium, hyperproliferation with increased epidermal cell turn-over, impaired healing of wounds, and increased transepidermal water loss. These skin alterations were reversible upon substitution. The principal sources of the essential fatty acids, which are classified by the position of their first double bond as either omega-3 or omega-6 fatty acids, are, primarily, cold-water fish (for omega-3 fatty acids) or vegetable oils (for omega-6 fatty acids). In mammals, the presence of different enzymes which give unsaturation and enzymes which give elongation can lead to the formation of additional secondary products.
The observation that populations that exhibit a high level of omega-3 fatty acid consumption (for example, Eskimos) exhibit only one-twentieth the incidence of psoriasis of comparable populations who nourish themselves primarily with omega-6 fatty acids, has led to several clinical studies which examined the effect of a diet rich in fish oil, that is, an oral application of fish oil, on the course of various forms of psoriasis (for example, The Lancet, Feb. 20, 1988, page 378; Journal of the American Academy of Dermatology, 1988, volume 18, pages 1267 through 1273; British Journal of Dermatology, 1987, 117, pages 599-613).
While the indications are not uniform for chronic, constant, common psoriasis, they do, however, agree on the fact that a clinical improvement results from a linear dosage/effect relationship. For the exudative forms (exanthematous psoriasis, pustular psoriasis), but also for psoriatic arthritis, the trend appears to be toward uniformly positive indications, although the published number of cases is still small. This therapeutic reasoning is based on the suppression and antagonization of the metabolism of arachidonic acid vital to the pathogenesis by inclusion of the structurally-related eicosapentaenoic acid (EPA) in the lipid metabolism of both keratinocytes as well as neutrophile granulocytes. Granulocytes seem to play an important role, particularly in inflammatory forms of psoriasis, a fact that is supported by increased function parameters as well as the histological characteristics of the infiltration of the epidermis and the formation of so-called Munroe's micro-abscesses. In particular in pustular forms, the increased chemotactic and pro-inflammatory activity results in the formation of clinically visible pustules on skin altered by inflammation.
As a potent chemotactic substance, LTB4, a lipoxygenase product of the arachidonic acid that has been found in increased levels in psoriatic lesions, can explain these findings. In addition, it stimulates keratinocyte proliferation in cell cultures.
The oral ingestion of eicosapentaenoic acid (omega-3 fatty acid) contained in fish oil, the metabolism of the arachidonic acid (omega-6 fatty acid) can be competatively inhibited to such an extent
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Burczyk, A., "Bedeutung unges attigter Fetts auren in Nahrung und Kosmetik," Seifen- Ole-Fette-Wachse 115:462-463 (1989). (Summary Only).
Chapkin, R. S. et al., "Dietary Influences of Evening Primrose and Fish Oil on the Skin of Essential Fatty Acid-Deficient Guinea Pigs," J. Nutrition 117:1360-1370 (Aug. 1987).
Horrobin, D. F., "Low Prevalances of Coronary Heart Disease (CHD), Psoriasis, Asthma and Rheumatoid Arthritis in Eskimos: Are They Caused by . . . ?," Medical Hypotheses 22:421-428 (Apr. 1987).
Lowe, N. J. et al., "Linoleic Acid Effects on Epidermal DNA Synthesis and Cutaneous Prostaglandin Levels in Essential Fatty Acid Deficiency," J. Invest. Dermatol. 70:200-203 (Apr. 1978).
Martinez, M. and Ballabriga, A., "Effects of Parenteral Nutrition with High Doses of Linoleate on the Developing Human Liver and Brain," Lipids 22:133-138 (1987).
Simopoulos, A. P., "Summary of the NATO Advanced Research Workshop on Dietary .omega.3 and .omega.6 Fatty Acids: Biological Effects and Nutritional Essentially," J. Nutrition 119:521-528 (Apr. 1989).
Ziboh, V. A. et al., "Effects of Dietary Supplementation of Fish Oil on Neutrophil and Epidermal Fatty Acids", Arch. Dermatol. 122:1277-1282 (Nov. 1986).
Grimminger Friedrich
Mayser Peter
Schlotzer Ewald
Seeger Werner
Sommermeyer Klaus
Frazier Barbara S.
Fresenius AG
Geist Gary
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