Injectable nitrogen mustard compositions comprising a cyclodextrin derivative and methods of making and using the same
AssigneeCyDex Pharmaceuticals, Inc.
InventorsJames D. Pipkin, Stephen G. Machatha
Life of this patent
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Abstract
The present disclosure is directed to pharmaceutical compositions comprising a nitrogen mustard and a cyclodextrin derivative, and methods of making and using the same.
Claims10
An injectable aqueous pharmaceutical formulation comprising 8.5 mL of an aqueous solution at a pH of 5, said solution consisting of 9 g/L sodium chloride, a sulfobutyl ether-β-cyclodextrin, and 5 mg/mL melphalan, wherein said sulfobutyl ether-β-cyclodextrin and said melphalan are present in a weight ratio of 54:1;
- and
- wherein said aqueous pharmaceutical formulation is stable at room temperature for at least one hour, as compared to a cyclodextrin-free reference melphalan standard.
An injectable aqueous pharmaceutical formulation comprising 10 mL of an aqueous solution with a pH of 5, said formulation consisting of a sulfobutyl ether-β-cyclodextrin and 0.45 mg/mL melphalan;
- wherein said sulfobutyl ether-β-cyclodextrin and said melphalan are present in a weight ratio of at least 54:1;
- and
- wherein said aqueous pharmaceutical formulation is stable at room temperature for at least 4 hours, as compared to a cyclodextrin-free reference melphalan standard.
An injectable aqueous pharmaceutical formulation comprising 8.5 mL of an aqueous solution at a pH of 5, said solution consisting of at least one of an antioxidant, preservative, or buffer, 9 g/L sodium chloride, a sulfobutyl ether-β-cyclodextrin, and 5 mg/mL melphalan, wherein said sulfobutyl ether-β-cyclodextrin and said melphalan are present in a weight ratio of 54:1;
- wherein said aqueous pharmaceutical formulation is stable at room temperature for at least one hour, as compared to a cyclodextrin-free reference melphalan standard.
An injectable aqueous pharmaceutical formulation consisting of 5 mg/mL melphalan, sulfobutyl ether-β-cyclodextrin and 9 g/L sodium chloride;
- wherein said sulfobutyl ether-β-cyclodextrin and said melphalan are present in a weight ratio of 54:1;
- wherein the aqueous pharmaceutical formulation has a pH of 5;
- wherein said aqueous pharmaceutical formulation is stable at room temperature for at least one hour, as compared to a cyclodextrin-free reference melphalan standard;
- and
- further wherein administering the formulation provides a melphalan AUC0-t in a subject that is at least 20% greater than a melphalan AUC0-t provided by a melphalan formulation containing an equivalent dose of melphalan and lacking the cyclodextrin derivative.
An injectable aqueous pharmaceutical formulation consisting of 0.45 mg/mL melphalan, sulfobutyl ether-β-cyclodextrin and 9 g/L sodium chloride;
- wherein said sulfobutyl ether-β-cyclodextrin and said melphalan are present in a weight ratio of at least 54:1;
- wherein the aqueous pharmaceutical formulation has a pH of 5;
- wherein said aqueous pharmaceutical formulation is stable at room temperature for at least 4 hours, as compared to a cyclodextrin-free reference melphalan standard;
- and
- further wherein administering the formulation provides a melphalan AUC0-t in a subject that is at least 20% greater than a melphalan AUC0-t provided by a melphalan formulation containing an equivalent dose of melphalan and lacking the cyclodextrin derivative.
Dependencies are inferred from the claim text.