Self-emulsifying composition of omega3 fatty acid

Abstract

A self-emulsifying composition contains: 70 to 90% by weight of at least one compound selected from the group consisting of ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters; 0.5 to 6% by weight of water; 1 to 29% by weight of a polyoxyethylene sorbitan fatty acid ester as an emulsifier (optionally including a polyoxyl castor oil, and not including lecithin); and lecithin in an amount of 3 to 40 parts by weight in relation to 100 parts by weight of ω3 polyunsaturated fatty acids and the like. The self-emulsifying composition is excellent in self-emulsifying property, composition dispersibility, emulsion stability, and absorbability, is free from ethanol and polyhydric alcohols or only has such an alcohol added thereto at a reduced concentration, and is useful for foods and pharmaceuticals.

Description

TECHNICAL FIELD[0001]This invention provides a self-emulsifying composition containing at least one member selected from the group consisting of ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters. This invention also provides its pharmaceutical product, its production method, a therapeutic method using such pharmaceutical product, and a method for using the same.BACKGROUND ART[0002]Known ω3 polyunsaturated fatty acids (hereinafter abbreviated as ω3 PUFA) include α-linolenic acid, eicosapentaenoic acid (hereinafter abbreviated as EPA), and docosahexaenoic acid (hereinafter abbreviated as DHA). Since the ω3 PUFA and pharmaceutically acceptable salts and esters thereof (hereinafter abbreviated as ω3 PUFA) have actions such as anti-arteriosclerosis action, platelet aggregation suppressive action, blood lipid lowering action, anti-inflammatory action, carcinostatic action, and central action, they are blended in various food products, and commercially s...

AI Technical Summary

Benefits of technology

[0194]The self-emulsifying composition of the present invention contains a small amount of water instead of the ethanol and the polyhydric alcohol in its composition. Compatibility of the composition improves by such composition, and amount of the emulsifier used can also be reduced, and accordingly, safety for animals (including human) is thereby improved. In addition, the ω3 PUFA will be included at a higher content, and this enables reduction in the amount of emulsifier used, and compliance is thereby improved.

[0195]Inclusion of the water in the composition also enables a composition without or with minimized use of the ethanol or the polyhydric alcohols, and hence, prevention of the softening of the capsule film, and deformation of the capsule. A preparation with minimized use of the ethanol and the polyhydric alcohols can also be obtained. A preparation which is excellent in drug compliance or drug adherence can also be obtained.

[0196]The self-emulsifying composition of the present invention is excellent in at least one of compatibility (appearance), self-emulsifying property, dispersibility of the composition, emulsion stability, and absorbability, is rapidly absorbed even if administered before the meal or after the low-fat meal to thereby suppress an increase in the serum TG after the meal, increases the ω3PUFA concentration in blood (the term “in blood” means “in whole blood, plasma, or serum” and this also applies to the following description), or is administered before going to bed to thereby prevent essential fatty acid deficiency upon administration of the lipase inhibitor.

[0197]The self-emulsifying composition of the present invention reduces the amount of the ω3PUFA that is not absorbed and then egested after administration, enhances tissue migration properties of the ω3PUFA, increases the uptake of ω3PUFA into phospholipid in blood, or alternatively decreases arachidonic acid in blood and / or improves the EPA / AA ratio.

[0198]The self-emulsifying composition enables not only the storage at room temperature but also the storage under the conditions of low temperature (for example, 5° C.) and high temperature (for example, 40° C.) without causing separation or cloudiness of the composition, namely, with good appearance. The self-emulsifying composition of the present invention is also excellent in at least one of self-emulsifying property, dispersibility of the composition, emulsion stability, and absorbability.

[0199]The self-emulsifying composition of the present invention has storage stability at at least one of room temperature, low temperature and high temperature, has storage stability at at least one specific temperature selected from the temperature of from, for example, 5° C. to 40° C., does not change the parameters to cause stable quality as a pharmaceutical product to deteriorate if stored in at at least one of room temperature, low temperature and high temperature, or does not change the parameters to cause stable quality as a pharmaceutical product to deteriorate if stored at at least one specific temperature selected from the temperature of from, for example, 5° C. to 40° C.

Problems solved by technology

However, dosage method or drug compliance has become a problem for those people not taking breakfast with the recent change in the life style, patients who can only take meals at a reduced amount, patients who can only take a fluid diet (milk, rice broth, starch gruel, egg, soup, juice, or oral nutritional supplement), patients with reduced absorption ability of the intestinal tract (for example, elderly, patients of intestinal disease, patients after intestinal surgery, terminal cancer patients, and patients taking a lipase inhibitor), or patients who are unable to take meals such as those after the cerebral infarction.

However, volatilization of the ethanol is associated with the risk of capsule deformation and bubble inclusion in the capsule, damages in the quality such as capsule deformation and cracks, as well as denaturing of the content in the capsule such as cloudiness and separation.

In addition, use of a preparation containing such composition should be impossible or difficult if not impossible for patients intolerable for the alcohol (ethanol).