Hydrolysis-optimized lipid emulsions and use thereof

Details Hydrolysis-optimized lipid emulsions and use thereof Hydrolysis-optimized lipid emulsions and use thereof

1998-03-12

1999-12-28

Harrison, Robert H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Radical -xh acid, or anhydride, acid halide or salt thereof...

514943, A61K 3119

Patent

active

060082488

DESCRIPTION:

BRIEF SUMMARY
The present invention pertains to hydrolysis-optimized isotonic lipid emulsions (fat emulsions) for parenteral administration, in particular for parenteral nutrition, and their use in situations of exaggerated inflammatory response (e.g. post-surgery, post-trauma, sepsis, inflammatory or wasting diseases) or of increased risk of vascular thrombosis and severe cardiac arrytlmia where it is important to avoid inflicting an exogeneous triglyceride accumulation while making free fatty acids available to different tissues of the body as rapidly as possible.
Lipid emulsions for parenteral nutrition serve to supply the body with fats in an intravenously acceptable dosage form when normal (oral) nutrition is impossible, compromised or medically contraindicated or when it is necessary to promptly modify the fatty acid pattern of the cells. The lipid emulsions currently available are prepared from vegetable oils (e.g. safflower or soybean oils); in some cases they also contain medium-chain triglycerides (MCT) and/or oils of marine origin (fish oils).
Long-chain triglycerides of vegetable or marine origin serve as an energy source and, when containing polyunsaturated fatty acids, as suppliers of essential fatty acids. The classification of such polyunsaturated fatty acids into omega-6 or omega-3 series types is based on chemical structural features, more precisely, on the distance of the first unsaturated bond from the methyl end (omega end) of the fatty acid molecule.
The vegetable oils, e.g. of soybean and safflower, are characterized by a high content of polyunsaturated fatty acids of the omega-6 series (predominantly linoleic acid, 18:2 n-6) whereas their content of omega-3 fatty acids (almost exclusively in the form of .alpha.-linolenic acid, 18:3 n-3) is low.
Fish oils obtained from cold-water fish are characterized by a high content of polyunsaturated fatty acids of the omega-3 series (predominantly eicosapentaenoic acid, EPA, 20:5 n-3, and docosahexenoic acid, DHA, 22:6 n-3) whereas their content of omega-6 fatty acids is low.
The medium-chain triglycerides administered with the lipid emulsions serve mainly as a source of energy. Medium-chain triglycerides do not contain any unsaturated fatty acids and hence contain neither omega-6 nor omega-3 essential fatty acids.
Numerous clinical observations underline the principal suitability of lipid emulsions for parenteral nutrition and for substituting essential fatty acids in severe diseases and the metabolic conditions involved.
The human body is itself incapable of producing the vital, polyunsaturated long-chain fatty acids of the omega-6 or omega-3 series; i.e. they have to be administered orally, enterally or parenterally. The body is only able to synthesize longer-chain unsaturated fatty acids from shorter-chain ones; formation of omega-6 fatty acids from precursors of the omega-3 series or vice versa is impossible, however.
Correspondingly, there is a need for lipid emulsions for parenteral administration which contain medium-chain triglycerides as well as triglycerides of omega-6 and omega-3 fatty acids as lipid components.
EP-A-0 311 091 describes isotonic lipid emulsions for parenteral nutrition comprising, in addition to conventional additives and auxiliary agents, omega-3 fatty acids, omega-3 fatty acids in the form of their esters or as components of fish oils, medium-chain triglycerides, as well as optionally at least one vegetable oil providing omega-6 fatty acids in a proportion of up to 30%, based on the lipid content of the emulsion.
DE-OS-37 21 137 describes lipid emulsions for parenteral nutrition comprising eicosapentaenoic acid triglyceride and/or docosahexaenoic acid triglyceride, or fish oils containing such triglycerides, as well as vegetable oils containing omega-6 fatty acids, and medium-chain triglycerides.
DE-OS-34 09 793 describes a lipid emulsion for transfusion comprising a fatty acid containing from 20 to 22 carbon atoms, esters thereof, or a mixture of 2 or more of such fatty acids or esters, as well as a vegetable oil, an emulsifie

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