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US 6,605,298 B1Granted
Pharmaceutical compositions and their use
AssigneePhares Pharmaceutical Research N.V.
InventorsSteven Leigh, Mathew L. S. Leigh
Life of this patent
Estimating the term…
Abstract
The invention provides a composition for delivering at least one biologically active compound to a living organism, said composition comprising at least one micelle-forming membrane lipid
Claims54
A unit dosage form of a biologically active compound for delivering said compound to a living organism, said dosage form comprising:
- the biologically active compound;
- a mixture of a bilayer-forming diacyl phospholipid with at least one micelle-forming monoacyl phospholipid, said mixture being obtained from enzymatic deacylation of a membrane phospholipid and said bilayer-forming diacyl phospholipid and said micelle-forming monoacyl phospholipid having a molar ratio in the range of 1:5 to 25:1;
- and 5% to 90% by weight of a mixture of a water-miscible hydrophilic medium which is pharmaceutically acceptable and a polyol, said mixture being capable of dissolving both the biologically active compound and the micelle-forming phospholipid, thus forming a homogeneous liquid, gel or semi-solid that has the property of yielding dispersed lipid aggregates upon contact or further dilution with an aqueous medium.
A liquid composition comprising:
- (a) a mixture of a bilayer-forming diacyl phospholipid with at least one micelle-forming monoacyl phospholipid;
- and
- (b) ethanol in an amount effective to mobilize the lipids;
- and/or
- (c) a polyol or a further pharmaceutically acceptable hydrophilic medium in an amount effective to maintain the lipids in solution at room temperature;
- said micelle-forming phospholipid and said bilayer-forming phospholipid are in a mixture resulting from enzymatic deacylation of a membrane phospholipid, said bilayer-forming diacyl phospholipid and said micelle-forming monoacyl phospholipid having a molar ratio in the range of 1:5 to 25:1, or are a blend of said deacylated phospholipid with pure micelle-forming phospholipid or membrane-forming phospholipid.
3 more elements
A liquid composition comprising:
- (a) a mixture of membrane phospholipids which comprises a micelle-forming monoacyl phospholipid and a bilayer-forming diacyl phospholipid;
- and
- (b) water;
- said micelle-forming phospholipid and said bilayer-forming phospholipid being in a mixture resulting from enzymatic deacylation of a membrane phospholipid, said bilayer-forming diacyl phospholipid and said micelle-forming monoacyl phospholipid having a molar ratio in the range of 1:5 to 25:1, or being a blend of said deacylated phospholipid with a pure micelle-forming phospholipid or membrane-forming phospholipid.
1 more element
A unit dosage form of a biologically active hydrophilic compound for delivering said compound to a living organism, said composition comprising:
- the biologically active compound;
- at least one micelle-forming monoacyl phospholipid in admixture with a bilayer-forming diacyl phospholipid, said admixture of phospholipids being enzymatically derived, and said bilayer-forming diacyl phospholipid and said micelle-forming monoacyl phospholipid in said admixture having a molar ratio in the range of 1:5 to 25:1;
- and
- a hydrophilic medium that dissolves both the biologically active compound and the admixture of phospholipids to form a homogenous liquid, gel or semi-solid that has the property of yielding dispersed lipid aggregates upon contact or further dilution with an aqueous medium.
1 more element
A composition for topical application for delivering a biologically active compound to a living organism, said composition comprising:
- the biologically active compound;
- at least one micelle-forming monoacyl phospholipid in admixture with a bilayer-forming diacyl phospholipid, said admixture of phospholipids being enzymatically derived, and said bilayer-forming diacyl phospholipid and said micelle-forming monoacyl phospholipid in said admixture having a molar ratio in the range of 1:5 to 25:1;
- and
- a hydrophilic medium that dissolves both, the biologically active compound and the admixture of phospholipids, to form a homogeneous liquid, gel or semi-solid that has the property of yielding dispersed lipid aggregates upon contact or further dilution with an aqueous medium.
1 more element
Dependencies are inferred from the claim text.