Formulation of insoluble small molecule therapeutics in lipid-based carriers
First Claim
1. A formulation comprising at least one unsaturated amphiphilic lipid and an amphipathic or hydrophobic drug or pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof wherein the drug and the lipid are present in a ratio ranging from between about 0.015 and about 0.15 on a mole/mole basis.
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Accused Products
Abstract
The present invention provides formulations containing at least one unsaturated amphiphilic lipid and an amphipathic or hydrophobic drug and methods of making these formulations. In particular, the present invention provides formulations of least one unsaturated phospholipid and an amphipathic or hydrophobic pyrimidine drug, methods of making these formulations and the use of such formulations in a variety of contexts, including, for example, the treatment of proliferative disorders, such as tumors and cancers.
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Citations
57 Claims
- 1. A formulation comprising at least one unsaturated amphiphilic lipid and an amphipathic or hydrophobic drug or pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof wherein the drug and the lipid are present in a ratio ranging from between about 0.015 and about 0.15 on a mole/mole basis.
- 37. A formulation comprising a pyrimidine derivative or pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof and an unsaturated amphiphilic lipid.
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39. A method of making a formulation, said method comprising the steps of:
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mixing at least one unsaturated amphiphilic lipid, an amphipathic or hydrophobic drug or pharmaceutically acceptable salts, hydrates, solvates, or N-oxides thereof and a solvent;
removing the solvent to form a residue comprising drug and lipid; and
mixing the residue with water or an aqueous solution;
wherein the drug and the lipid are present in a ratio ranging from between about 0.015 and about 0.15 on a mole/mole basis. - View Dependent Claims (40, 41, 42, 43, 44, 45, 46, 47)
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48. A formulation made by a process comprising the steps of:
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mixing at least one unsaturated amphiphilic lipid, an amphipathic or hydrophobic drug or pharmaceutically acceptable salts, hydrates, solvates, or N-oxides thereof and a solvent;
removing the solvent to form a residue comprising drug and lipid; and
mixing the residue with water or an aqueous solution;
wherein the drug and the lipid are present in a ratio ranging from between about 0.015 and about 0.15 on a mole/mole basis.
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Specification