Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1993-12-29
1995-07-18
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514552, 514558, 514560, A61K 3166
Patent
active
054341833
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/SE92/00333, filed May 19, 1992.
Introduction
The present invention relates to emulsions containing phospholipids of marine and/or synthetic origin with a high mount of (at least 30% (w/w) of its total fatty acid content) omega-3 (hereinafter written as) w3-fatty acids, with docosahexaenoic acid, 22:6w3 (hereinafter written as DHA) and eicosapentaenoic acid, 20:5w3 (hereinafter written as EPA) in combination, as well as the use of these phospholipids. The phospholipids are used as emulsifiers, nutritive substrates, as a pharmacologically active agent in an emulsion, as a component in pharmaceutical compositions or as a component in lipid particles.
Background of the Invention
It is known that lipid emulsions can be used intravenously to constitute an energy dense caloric source and a source of essential fatty acids for those patients who have difficulties in using orally administered nutrition.
Since the beginning of the 1960s, fat emulsions which are intended for intravenous nutrient supply and which exhibit insignificant secondary effects have been available (Wretlind, A. Development of fat emulsions, JPEN 5: No 3,230-35, 1981).
This developmental work has investigated the effect of emulsions which contain a number of different fats, such as soy bean oil, maize oil, safflower oil, cottonseed oil etc. and different emulsifiers, such as soy bean phospholipids, egg yolk phospholipids etc.
Emulsions for nutritive or therapeutic use are, for example, described in U.S. Pat. No. 4,168,308.
The nutritive emulsions now most commonly used contain a vegetable oil such as soybean oil and/or safflower oil, an emulsifying agent such as an egg yolk phospholipid and water together with glycerol. An example of such an emulsion is Intralipid.RTM., manufactured since 1962 and sold by Kabi Pharmacia AB. Intralipid.RTM. 10% contains 10% oil as soy bean oil and 1,2% egg yolk phospholipids.
Different fatty acids in the lipids have different physiological, biochemical and pharmacological properties and during the last years great interest has been concentrated on the importance of the w3-fatty acids, containing 18-22 carbon atoms.
The w3-fatty acids eicosapentaenoic acid (20:5w3, EPA) and docosahexaenoic acid (22:6w3, DHA) are essential fatty acids in man. Besides their nutritional value, they are also known to possess pharmacological effects. The most known and important are the cardiovascular effects, the beneficial effects on inflammatory and autoimmune diseases and the necessity of these fatty acids for the normal development of brain and retina functions.
These effects have such unimportance that a lot of work has been done to find good nutritional compositions containing a high mount of w3-fatty acids. See e.g. WO 87/02247 (Baxter) and U.S. Pat. No. 4,820,731 (New England Deaconess Hospital) in which marine oils are used which contain a high amount of the w3-fatty acids EPA and DHA.
The patient also needs omega-6 fatty acids (hereafter written as w6-fatty acids) which are found, for example, in vegetable oils. Nutrients given to patients should therefore also contain an appropriate vegetable oil. Infusion of lipid emulsions containing w6-fatty acids results, however, in a raised level of cholesterol and triglycerides in some patients, which should be avoided. Until now some patients depending on parenteral nutrition have not been able to avoid a certain increase of total cholesterol and triglycerides when an emulsion containing mainly w6-fatty acids is given. w6-Fatty acids also increase the level of eicosanoides and leucotrienes, which when overproduced in some patients, e.g. with overactive inflammatory and immunological reactions, may have deleterious effects.
Phospholipids containing EPA or DHA are known as being useful in various fields, such as foods, cosmetics, medicines, agriculture etc. and different methods for their-manufacture have been disclosed. See e.g. JP 2097393 and JP 1050890.
The use of phospholipids, containing EPA or DHA, as emulsifier for an EPA-triglyceride-emul
REFERENCES:
patent: 4820731 (1989-04-01), Mascioli et al.
Production of Health Food Egg, JP 59-39258 (Abstract), vol. 8, No. 126 (C-228) (1984).
Carcinostatic Agent, JP 62-77319 (Abstract), vol. 11, No. 273 (C-445) (1987).
Love, et al., Specific accumulation of cholesterol-rich liposomes in the inflammatory tissue of rats with adjuvant arthritis, Annals of the Rheumatic Diseases, 1990, vol. 49, pp. 611-614.
Hamazaki, et al., Injection of Tridocosahexaenoyl-Glycerol Emulsion and Fatty Acid Composition of Blood Cells, Lipids, 1987, vol. 2(12), pp. 1031-1034.
Hamazaki, et al., The Infusion of Trieicosapentaenoyl-Glycerol into Humans and the In Vivo Formation of Prostaglandin I.sub.3 and Thromboxane A.sub.3, Biochem. Biophys. Res. Commun., 1988, vol. 151(3), pp. 1386-1394.
Billiar, et al., Fatty acid intake and Kupffer cell function: Fish oil alters eicosanoid and monokine production to endotoxin stimulation, Surgery, 1988, vol. 104(2), pp. 343-349.
Urakaze, et al., Infusion of Emulsified Trieicosapentaenoyl-Glycerol into Rabbits--The Effects of Platelet Aggregation, Polymorphonuclear Leukocyte Adhesion, and Fatty Acid Composition in Plasma and Platelet Phospholipids, Thrombosis Research, 1986, vol. 44, pp. 673-682.
Childs, et al., Divergent lipoprotein responses to fish oils with various ratios of eicosapentaenoic acid and doc sahexaenoic acid.sup.1-3, Am. J. Clin. Nutr., 1990, vol. 52, pp. 632-639.
Pharmacia AB
Raymond Richard L.
LandOfFree
Phospholipids containing omega-3-fatty acids does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Phospholipids containing omega-3-fatty acids, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Phospholipids containing omega-3-fatty acids will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2419148