Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1991-12-09
1994-10-04
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514861, A61K 3120
Patent
active
053527003
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the use of essential fatty acids having 18-20 carbon atoms in the preparation of a drug for the treatment of infantile seborrhoeic eczema and asteatotic eczema.
Essential fatty acids are long-chained unsaturated fatty acids acids which cannot be synthetized in the body but must be provided via food.
Linoleic acid, which is the essential fatty acid having the shortest chain, metabolizes by elongating and desaturating via gammalinolenic acid and dihomogammalinolenic acid to arachidonic acid, which is a precursor for prostaglandin E.sub.2, PGE.sub.2.
It is known that a deficiency of PGE.sub.2, which inter alia comprises a transport ligand for zinc in the mucous membrane of the intestines, brings about reduced zinc absorption in humans and that the enzyme delta-6-desaturas, D-6-D, is zinc dependent.
By testing on animals it has been shown that desaturating of linoleic acid to gammalinolenic acid mediates via D-6-D.
Linoleic acid (.omega.-6-C18:2) hence desaturates via D-6-D to gammalinolenic acid (.omega.-6-C18:3), which elongates to dihomogammalinolenic acid (.omega.-6-C20:3), which in its turn via the enzyme D-5-D, desaturates to arachidonic acid (.omega.6-C20:4).
Since the essential fatty acids, which via food are provided to humans, consist almost entirely of linoleic acid, the amount of the essential fatty acids gammalinolenic acid, dihomogammalinolenic acid and arachidonic acid metabolized in the body will successively decrease if the activity of D-6-D is reduced or stopped.
In studies of experiments with animals it has been shown that D-6-D-activity in rat fetuses is very low. The state in humans is unknown.
There are no reported cases of naturally occurring deficiency of essential fatty acids in humans.
The function and importance of linoleic acid in the skin is that it is incorporated in the membranes and enzymes, it is important for the barrier functions of the skin (permeability and absorption) and that lack of linoleic acid results in a defective shield in the horny layer.
The function and importance of arachidonic acid is that it is incorporated in the phospholipides of the skin (lecithin, phosphatidylethanolamine) and it is a precursor for prostaglandins which regulate the balance of epidermis and mediate inflammation. Lack of arachidonic acid in the skin affects the regulation of the horny layer and of inflammatory conditions.
Deficiency of essential fatty acids, however, has been described as a post-operative effect in surgery and as a secondary effect of manipulation of the diet. The manifestation of the skin in said deficiency has then been that of dry, scaly, leathery-like inflamed skin conditions. Oozing, secondarily-infected lesions mainly in body folds are usually apparent. Furthermore, an increased transepidermal water loss has been observed.
In studies regarding skin changes due to zinc deficiency in infants two clinically distinctive types have been observed:
1) The classic zinc deficiency dermatitis with low zinc value in serum. These infants all had a low zinc intake due to a low zinc content in their mothers breastmilk. The skin changes were primarily localised in the diaper region, the face, the back of the hands and the feet with quite distinctively demarcated plaques, in some places heavily scaling, almost of psoriasis form type. These children responded promtly and well to applied zinc substitute.
2) The symptoms often first appeared in 3-6 weeks old infants starting in the diaper region, where skin changes were more confluent. Furthermore, round to oval reddish, somewhat thickened, lightly scaling patches could be seen. The scalp was covered by a thick, yellow-brown, somewhat greasy desquamation. In body folds, armpits and behind the ears, red, oozing lesions could be seen, often secondarily infected.
Type 2) on analysis of essential fatty acids in serum has been shown to have a pattern that corresponds to a defectively functioning D-6-D. These children had a slightly decreased zinc value in serum, which is thought to be a side effect due to red
REFERENCES:
patent: 4444755 (1984-04-01), Horrobin et al.
Sakai, Keiko, Ueno, Kohji, Ogawa, Yunosuke, and Okuyama, Harumi, "Fatty Acid Compositions of Plasma Lipids in Young Atopic Patients", Chem. Pharm. Bull., vol. 34, No. 7, pp. 2944-2949, Feb. 6, 1986.
The Williams & Wilkins Co., "Arachidonic Acid and Leukotrienes in Dermatology", The Journal of Investigative Dermatology, vol. 81, No. 34, pp. 293-296, 1983.
Manku, Mehar S., Horrobin, David F., Morse, Nancy, Kyte, Vicki, and Jenkins, Kenneth, "Reduced Levels of Prostaglandin Precursors in the Blood of Atopic Patients: Defective Delta-6-Desaturase Function as a Biochemical Basis for Atopic", Prostaglandins Leukotrienes and Medicine, vol. 9, pp. 615-528, 1982.
Galland, Leo, "Increased Requirements for Essential Fatty Acids in Atopic Individuals: A Review with Clinical Decriptions", Journal of the American College of Nutrition, vol. 5, pp. 213-228, 1986.
Wright et al., Chemical Abstracts 111(25):230059r, 1989.
Bordoni et al., Biosis 88:400775, BA86:73414, 1988.
Biagi et al., Biosis 88:400774, BA86:73413, 1988.
Frithz Anders
Tollesson Anders
Cintins Marianne M.
Jarvis William R. A.
LandOfFree
Use of essential fatty acids for the preparation of a drug for t does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Use of essential fatty acids for the preparation of a drug for t, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Use of essential fatty acids for the preparation of a drug for t will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-581571