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US 5,747,066 AGranted
Mixed micelles
AssigneeHoffmann-La Roche Inc.
InventorsFolker Pittrof, Hans Steffen
Life of this patent
Estimating the term…
Abstract
Mixed micelles for the aqueous solubilization of active substances which are difficultly soluble or insoluble in water with improved storage properties consist of a phosphatide having saturated, branched fatty acid residues and a bile acid salt or dihexanoyllecithin.
Claims44
A fluid mixed micelle composition containing micelles dispersed in an aqueous media wherein said micelles comprise:
- a) a first compound which is a phosphatide in which two of the hydroxyl groups of the glycerol moiety of said phosphatide are esterified with:
- residues formed from saturated fatty acids which independently contain a straight chain of from14 to 20 carbon atoms and one or both of said fatty acids is substituted at one to three carbon atoms with C.sub.1-5 -alkyl, and
- b) a second compound which is a bile acid salt or dihexanoyllecithin,
- wherein the concentration of the first compound in said composition is in the range from about 1 mg/ml to about 200 mg/ml and the molar ratio of the first compound to the second compound in said composition is in the range from 0.1:1 to 2:1;
- or a lyophilozate of said composition.
2 more elements
A method of making a mixed micelle composition comprising dissolving in an aqueous media:
- a) a first compound which is a phosphatide in which two of the hydroxyl groups of the glycerol moiety of said phosphatide are esterified with:
- residues formed from saturated fatty acids which independently contain a straight chain of from 14 to 20 carbon atoms and one or both of said fatty acids is substituted at one to three carbon atoms with C.sub.1-5 -alkyl, and
- b) a second compound which is a bile acid salt or dihexanoyllecithin,
- wherein the concentration of the first compound in said composition is in the range from about 1 mg/ml to about 200 mg/ml and the molar ratio of the first compound to the second compound in said composition is in the range from 0.1:1 to 2:1.
1 more element
Dependencies are inferred from the claim text.