US 5,626,873 AGranted

Emulsions

AssigneeThe Liposome Company, Inc.

InventorsAlan L. Weiner, Sharon Carpenter-Green

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Abstract

A novel oil and water emulsion useful for delivery of a bioactive agent is disclosed. The emulsion comprises a first HLB requirement amount of surfactant dioleoyl phosphatidylethanolamine. In particular embodiments the emulsion includes a secondary surfactant other than dioleoyl phosphatidylethanolamine except in the limiting case wherein the HLB requirement is the HLB value of dioleoyl phosphatidylethanolemine in which case the the HLB requirement amount of a secondary surfactant is 0. By appropriate selection of dioleoyl phosphatidylethanolamine to secondary surfactant ratios, it is possible to prepare emulsions for pharmaceutical delivery of a bioactive agent using an oil phase having a required HLB value up to about 17.4. Above a required HLB value of about 17.4. dioleoyl phosphatidylethanolamine may be used to reduce the amount of secondary surfactant required to form an emulsion.

Claims12

Dependent claims

A method of administering a bioactive agent to a mammal by parenterally administering to the mammal a composition comprising an emulsion which comprises:

(a) the bioactive agent;
(b) water;
(c) a pharmaceutically acceptable oil having an HLB requirement of between about 8 and less than about 17.4;
and,
(d) a phospholipid surfactant comprising from about 5% to about 30% (w/w) of the emulsion and providing an HLB value equal to the HLB requirement of the oil,
wherein dioleoyl phosphatidylethanolamine and a phosphatidylcholine having an HLB value of about 7.6 comprise 100% by weight of the phospholipid surfactant;
wherein the weight percentage of dioleoyl phosphatidylethanolamine in the phospholipid surfactant and is from about 4.1% by weight of the phospholipid surfactant to less than 100% by weight of the surfactant;
and,
wherein the weight percentage of the phosphatidylcholine in the phospholipid surfactant is equal to 100% by weight of the surfactant minus the weight percentage of dioleoyl phosphatidylethanolamine in the surfactant and is from greater than about 0% by weight of the surfactant to at most about 95.9% by weight of the surfactant.

6 more elements

Dependencies are inferred from the claim text.

Facts

Application: 08/442,080Filed 16 May 1995 · continuation
Priority: 3 Mar 1989
Granted: 6 May 1997
Term ends: Not estimatedThe source records don’t support an estimate.

Classification5 codes

A61K 9/0026
Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in…
A61K 9/0014
Galenical forms characterised by the site of application: skin, i.e. galenical aspects of topical compositions
A61K 9/0019
Galenical forms characterised by the site of application: injectable compositions; Intramuscular, intravenous, arterial, subcutaneous…
A61K 47/24
Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite: containing atoms other than carbon,…