Organic compounds -- part of the class 532-570 series – Organic compounds – Fatty compounds having an acid moiety which contains the...
Patent
1997-06-11
1999-02-09
Geist, Gary
Organic compounds -- part of the class 532-570 series
Organic compounds
Fatty compounds having an acid moiety which contains the...
554103, 554223, 554224, 514553, 514554, C07C10100
Patent
active
058697144
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP95/01075, filed Mar. 22, 1990.
FIELD OF THE INVENTION
The present invention relates to salts of omega-3 polyunsaturated fatty acids and pharmaceutical formulations containing them.
SUMMARY OF THE INVENTION
In particular, the present invention relates to salts of C.sub.20 -C.sub.22 omega-3 polyunsaturated acids with aminoalcohols, having the following general formula (I) polyunsaturated acid; radical wherein n is 2 or 3.
Long-chain polyunsaturated fatty acids, in particular the omega-3 polyunsaturated acids have been found to be extremely important in the prevention and treatment of various morbid forms, in particular those connected with the cardiocirculatory system (platelet antiaggregatory action, thrombolytic action, antiatheromatous action and so on--see A. Leaf and P. C. Weber, New England J. Medicine, 318, 549, 1988), inflammatory pathologies (S. M. Prescott, J. Biol. Chem., 259, 7615, 1984) and some cancer forms (H. O. Bang et al., Acta Med. Scand., 220, 69, 1976). Marked efficacy was also demonstrated in the treatment of hypertriglyceridemia and hypercholesterolemia, of psoriasis, of immunology, learning and memory disorders, of central and peripheral nervous system pathologies, etc. These activities are often stimulated, at a biochemical level, by competition of the acids in question with arachidonic acid and metabolites originating therefrom through the effect of cyclo-oxygenase and lipoxygenase enzymes (prostaglandins, prostacyclin, thromboxanes and leukotrienes). In other cases the effect is simply attributed to the accumulation of polyunsaturated acids, replacing acids saturated or with a minor degree of unsaturation, in various organ and cell districts (plasma, platelet and RBC membrane, nervous system etc.).
Of the polyunsaturated fatty acids mentioned above, 4,7,10,13,16,19-cisdocosahexaenoic acid (hereinafter referred as DHA) and 5,8,11,14,17-ciseicosapentaenoic acid (hereinafter referred as EPA) are by far the most important. These acids are also found in marine algae as well as in various microorganisms, but, above all, in fish oils which are at present the commercial source of these polyunsaturated substances. Fish oils are known to contain DHA and EPA in a mixture with saturated and not so unsaturated acids, in the form of triglycerides and it is in this form that the material is at present commercially available for dietary or therapeutic uses (see for instance Maxepa.RTM. Seven Seas Health Care Ltd., Hull, England; R. I. Sterling et al., J. Immunol., 139, 4186, 1987). The contents in EPA and DHA in these glycerides is of about 30% expressed as the sum total of the two constituents.
Other dietary or therapeutic preparations of DHA and EPA (W. S. Harris, J. Lipid Res., 30, 785, 1989) were obtained by transesterification of the triglycerides with ethanol and subsequent concentration by different techniques and are therefore used as concentrate mixtures of EPA ethylester and DHA ethylester.
From a pharmaceutical point of view said long chain polyunsaturated fatty acids, as well as, generally speaking, all the derivatives thereof including their ethyl esters, are all extremely water insoluble oils, often dispensed in dosage form of soft gelatin capsules, thus making impossible to attain several pharmaceutically suitable formulations.
The use of organic solvents to incorporate triglycerides and esters in the aqueous phase would be, as such, inadvisable from the toxicological viewpoint and would not permit, at any rate, diluting the preparation in water owing to the consequent separation of the oleaginous phase. In particular, the alkaline and earth-alkaline metal salts, lead to strongly basic solutions, conseguently having a poor tolerance, and to the additional disadvantage of a concentration-related pH and an otter uncalled for supply of metal ions.
It has been now surprisingly found that great and unexpected advantages at the level of pharmaceutical technology as well as of a biological and pharmacological type can be attained by using salts of C
Carr Deborah D
Geist Gary
Prospa B.V.
Schneider Walter H.
LandOfFree
Salts of omega-3-polyunsaturated fatty acids and pharmaceutical does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Salts of omega-3-polyunsaturated fatty acids and pharmaceutical , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Salts of omega-3-polyunsaturated fatty acids and pharmaceutical will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1950174