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Claims for Patent: 5,559,148

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Claims for Patent: 5,559,148

Title: Parenteral busulfan for treatment of malignant disease
Abstract:Stable parenteral formulations of busulfan for parenteral administration are disclosed. The improved bioavailability of the parenteral formulations optimizes high dose busulfan therapy against malignant disease and improves the safety of such therapy.
Inventor(s): Andersson; Borje S. (Houston, TX), Bhagwatwar; Harshal P. (Houston, TX), Chow; Diana S. (Houston, TX)
Assignee: Board of Regents, The University of Texas System (Austin, TX) University of Houston-University Park (Houston, TX)
Application Number:08/449,685
Patent Claims: 1. A method for treating malignant disease responsive to busulfan in an individual comprising parenterally administering a pharmaceutically effective amount of busulfan dissolved in a solvent comprising water and a water miscible, physiologically acceptable, busulfan solvent.

2. The method of claim 1 where the administering is intravascular.

3. The method of claim 1 where the administering is intravenous.

4. The method of claim 1 wherein the water miscible, physiologically acceptable, busulfan solvent is N',N-dimethylacetamide.

5. The method of claim 4 wherein N',N-dimethylacetamide is at a concentration of 5% to 99%.

6. The method of claim 1 wherein the busulfan solvent is an aqueous polyethyleneglycol solution.

7. The method of claim 6 wherein polyethyleneglycol is at a concentration of about 5% to 50%.

8. The method of claim 6 wherein the polyethyleneglycol has a molecular weight between 200 and 2000.

9. The method of claim 6 wherein the polyethyleneglycol has a molecular weight between 350 and 450.

10. The method of claim 1 wherein the water miscible, physiologically acceptable, busulfan solvent is a mixture of N'N-dimethylacetamide and an aqueous carrier solution allowing busulfan solubility and stability.

11. The method of claim 10 wherein the aqueous carrier solution allowing busulfan solubility and stability is a polyethyleneglycol solution.

12. The method of claim 1 where the dissolved busulfan is at a concentration of 1-15 mg/ml.

13. A pharmaceutically acceptable formulation for parenteral administration of busulfan comprising busulfan dissolved at a concentration of 1-15 mg/ml in a mixture of a water miscible, physiologically acceptable, busulfan solvent and water.

14. The formulation of claim 13 wherein the water miscible, physiologically acceptable, busulfan solvent is N',N-dimethylacetamide.

15. The formulation of claim 14 wherein N',N-dimethylacetamide is at a concentration of 5% to 99%.

16. The formulation of claim 13 wherein the water miscible, physiologically acceptable, busulfan solvent is an aqueous polyethyleneglycol solution.

17. The formulation of claim 16 wherein polyethyleneglycol is at a concentration of 5% to 50%.

18. The formulation of claim 16 wherein the polyethyleneglycol has a molecular weight between 200 and 2000.

19. The formulation of claim 16 wherein the polyethyleneglycol has a molecular weight between 350 and 450.

20. The formulation of claim 13 wherein the mixture is a mixture of N',N-dimethylacetamide and an aqueous carrier solution allowing busulfan solubility and stability.

21. The formulation of claim 20 wherein the aqueous carrier solution allowing busulfan solubility and stability is a polyethyleneglycol solution.

22. The formulation of claim 13 wherein the water miscible, physiologically acceptable, busulfan solvent is propylene glycol.

23. The formulation of claim 13 wherein the water miscible, physiologically acceptable, busulfan solvent is an aqueous solution of hydroxypropylbetacyclodextrin.

24. A method of preparing a pharmaceutically acceptable formulation for parenteral administration of busulfan, the method comprising the steps of:

dissolving busulfan in a water miscible, physiologically acceptable, busulfan solvent to yield a busulfan working solution; and

diluting the busulfan working solution with an aqueous carrier solution allowing busulfan solubility and stability to yield a pharmaceutically acceptable, formulation for parenteral administration of busulfan.

25. The method of claim 24 wherein the aqueous carrier solution allowing busulfan solubility and stability is a polyethyleneglycol solution.

26. The method of claim 24 where the busulfan working solution has a concentration of busulfan of 1-75 mg/ml.

27. A method of preparing a pharmaceutically acceptable formulation for parenteral administration of busulfan, the method comprising the step of dissolving busulfan at a concentration of 1-75 mg/ml in a water miscible, physiologically acceptable, busulfan solvent.

28. The method of claim 24 or 27 wherein the water miscible, physiologically acceptable, busulfan solvent is N',N-dimethylacetamide.

29. The method of claim 28 wherein N',N-dimethylacetamide is at a concentration of 5% to 99%.

30. The method of claim 27 wherein the water miscible, physiologically acceptable, busulfan solvent is an aqueous polyethyleneglycol solution.

31. The method of claim 30 or 25 wherein the polyethyleneglycol is at a concentration of about 5% to 50%.

32. The method of claim 30 or 25 wherein the polyethyleneglycol has a molecular weight between 200 and 2000.

33. The method of claim 30 or 25 wherein the polyethyleneglycol has a molecular weight between 350 and 450.

34. A method for treating a patient undergoing a bone marrow transplant, the method comprising:

administering an intravascularly administrable busulfan preparation to a patient in an amount conditioning the patient for the bone marrow transplant, wherein the preparation comprises busulfan dissolved in a mixture comprising water and a water miscible, physiologically acceptable, busulfan solvent.

35. The method of claim 34 wherein the amount of busulfan administered is about 1 mg/kg every 6 hours.

36. The method of claim 34 wherein the amount of busulfan administered is up to about 380 mg daily.
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