Oil-in water emulsions

Details Oil-in water emulsions Oil-in water emulsions

1996-07-15

1997-11-18

Mosley, Terressa

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Liposomes

424 45, 424 84, 424498, 424501, 4284022, 436829, 514963, 514965, 514966, 514974, A61K 9127

Patent

active

056885288

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to oil-in-water type emulsions comprising a polar lipid material as an emulsifier. These emulsions are suitable for use as carriers for an active substance in a pharmaceutical composition, but also in nutritional, cosmetical, food and agricultural products.
1. Background of the Invention
Emulsions of the type oil-in-water for pharmaceutical applications, such as clinical nutrition and for the administration of lipophilic drugs, are generally based on natural lipids. The oil is typically a vegetable oil such as soybean oil, safflower oil or medium-chain triacylglycerol (MCT) oil. The emulsifier is typically a phospholipid such as egg yolk phospholipids (egg lecithin) or soybean phospholipids (soy lecithin). These emulsifiers consist of mixtures of phospholipid classes, such as phosphatidylcholine and phosphatidylethanolamine, which are zwitter-ionic, and phosphatidylinositol, which is anionic. It is widely common knowledge that these lecithin emulsifiers are the most utilised natural lipids in preparing emulsions on an industrial scale of the kind mentioned above. It is also well-known that such emulsions suffer from disadvantages and problems which relate to the emulsifier being phospholipids. Such disadvantages and problems are, for example, broad particle size distributions and particle fusions resulting in so-called creaming.
Most commercial fat emulsions are based on egg phospholipids, which are produced from animal sources, in most cases egg yolk powder. Animal sources are, in some cases, related to problems connected to virus contamination, and, in the specific case of egg yolk powder, bacteria such as Salmonella. Another important feature of egg phospholipids is the content of polyunsaturated fatty esters, such as arachidonate and docosahexaenoate, which are extremely susceptible to oxidation in the presence of even small amounts of oxygen. Thus, the odour and taste of egg phospholipids are often very unpleasant, which can be carried through to the fat emulsions. Contamination and oxidation may often cause problems which relate to industrial safety and handling aspects.
2. Prior Art
EP-A2-0 402 090 discloses an edible oil-in-water emulsion suitable for creams and dressings comprising 10-99% of the entire oil and fat content of a diglyceride mixture. In order to improve the stability the emulsion can also include 0.1-10%, based on the oil phase, of phospholipids.
EP-A2-0 391 369 discloses a stable pharmaceutical composition of an oil-in-water emulsion type which comprises an effective amount of a lipophilic drug. The emulsion is composed of 3-50% of an oily carrier, mainly MCT oil, 0.05-20% of a phospholipid, 0.03-10% of a non-ionic surfactant, and 0.05-50% of an ionic surfactant. The improved stability is said to be caused by a synergism between the stated ingredients.
Glycosylglycerides are a type of glycolipids which are well-known constituents of plant cell membranes. Two types based on galactose are very common, monogalactosyldiacylglycerol, MGDG, and digalactosyldiacylglycerol, DGDG, representing up to 40% of the dry weight of the thylakoid membranes.
Plant glyoolipids have carbohydrate units, mainly of galactose, linked to glycerol. In MGDG the 1-position of the galacrose ring has a .beta.-link to glycerol, and in DGDG there is an .alpha.,1-6 bond between the sugars. A minor constituent is the plant sulpholipid, more correctly named sulphoquinovosyldiacylglycerol, SQDG, which contains a sulphonate rather than a hydroxyl group linked to carbon 6 of the terminal deoxyglucose residue. Most plant glycolipids can be described by the general formula ##STR1## wherein R.sub.1 and R.sub.2 independently of each other are saturated or unsaturated fatty acid residues of 2-24 carbon atoms and 0-6 double bonds, further esterified hydroxy acids, that is estolides, or hydrogen; the carbohydrate is a monosaccharide unit; n=1-5; and R.sub.3 is a hydroxyl or sulphonate group.
In investigating the interaction of glycosylglycerides with water and other polar solvents we have

REFERENCES:
patent: 4610868 (1986-09-01), Fountain et al.
patent: 5151272 (1992-09-01), Engstrom et al.

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