Ibuprofen salt emulsifiers and cream formulations containing same
OwnerScott Krauserinventor
Life of this patent
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Abstract
Emulsions and creams containing ibuprofen effective for topical administration of the ibuprofen are provided without the presence of conventional O/W emulsifying agent. The emulsions and creams are formed by using the ibuprofen, in the form of its salt, as the O/W emulsifying agent. A minor amount of a W/O emulsifying agent may be included in the composition. Percutaneous delivery of ibuprofen is improved by using a skin penetration enhancing compound, such as 2-n-nonyl-1,3-dioxolane or decanaldimethyl acetal, as the oily phase of the emulsion.
Claims23
An ibuprofen O/W emulsion composition comprising:
- an emulsifying effective amount of ibuprofen salt as substantially the only O/W emulsifier;
- oily substance;
- and water.
A cream formulation effective for the topical administration of ibuprofen, comprising,
- an emulsifying and therapeutically effective amount of ibuprofen,
- a base effective for forming an ibuprofen salt,
- an oily substance,
- thickener and water,
- wherein the ibuprofen salt is present in an amount effective to form an oil-in-water emulsion without assistance of other emulsifying agent.
An ibuprofen emulsion consisting essentially of
- from about 1 to 10% by weight of ibuprofen,
- from about 0.3 to about 5% by weight of a basic substance selected from the group consisting of sodium hydroxide, triethanolamine, and diisopropanolamine,
- from about 5 to 10% by weight of oily skin penetration enhancing compound selected from the group consisting of 2-n-nonyl-1,3-dioxolane, decanaldimethyl acetal, isopropyl myristate, 1-dodecylazacycloheptan-2-one and pentadecalactone,
- 0 to about 3% by weight of secondary W/O emulsifying agent,
- 0 to 2% by weight of preservative,
- 0 to 1% by weight of odorant,
- 0 to 1% by weight of colorant, and
- balance water.
An ibuprofen cream consisting essentially of
- from about 1 to 10% by weight of ibuprofen,
- from about 0.3 to about 5% by weight of a basic substance selected from the group consisting of sodium hydroxide, triethanolamine, and diisopropanolamine,
- from about 5 to 10% by weight of oily skin penetration enhancing compound selected from the group consisting of 2-n-nonyl-1,3-dioxolane, decanaldimethyl acetal, isopropyl myristate, 1-dodecylazacycloheptan-2-one and pentadecalactone,
- a cream forming effective amount of thickening agent,
- 0 to about 3% by weight of secondary W/O emulsifying agent,
- 0 to 2% by weight of preservative,
- 0 to 1% by weight of odorant,
- 0 to 1% by weight of colorant, and
- balance water.
A method for preparing an ibuprofen containing emulsion without addition of O/W emulsifying agent, comprising
- combining ibuprofen with water, oily substance and a base in an amount effective to partially neutralize the carboxylic group of ibuprofen, and
- mixing the resulting combination until an O/W emulsion is formed.
A method for preparing an ibuprofen cream which does not contain any or only insubstantial amount of O/W emulsifying agent, which comprises,
- combining ibuprofen with water, oily substance and a base in an amount effective to partially neutralize the carboxylic group of ibuprofen, and
- mixing the resulting combination until an O/W emulsion is formed, and
- mixing the resulting emulsion with a thickening agent.
Dependencies are inferred from the claim text.