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Claims for Patent: 5,430,057

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Claims for Patent: 5,430,057

Title: Parenteral busulfan for treatment of malignant disease
Abstract:Stable parenteral formulations of busulfan safe for parenteral administration are disclosed that exhibit improved bioavailability and optimize high dose busulfan therapy against malignant disease.
Inventor(s): Andersson; Borje S. (Houston, TX), Bhagwatwar; Harshal P. (Houston, TX), Chow; Diana S. L. (Houston, TX)
Assignee: Board of Regents, The University of Texas System (Austin, TX) University of Houston-University Park (Houston, TX)
Application Number:08/129,995
Patent Claims: 1. A pharmaceutically acceptable formulation for intravascular administration of busulfan comprising busulfan dissolved at a concentration of about 1-19 mg/ml in a liquid mixture comprising water and about 10-70% of at least one miscible, physiologically acceptable, busulfan solvent selected from the group consisting of N',N-dimethylacetamide, polyethylene glycol, propylene glycol, glycerin cyclodextrin and hydroxypropylbetacyclodextrin.

2. A method for treating malignant disease responsive to busulfan in an individual comprising intravascular administration of a pharmaceutically effective amount of the formulation of claim 1.

3. The method of claim 2 where the administration is intravenous.

4. The method of claim 2 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 70%.

6. The method of claim 2 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 2 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 formulation of claim 8 wherein the water miscible, physiologically acceptable, busulfan solvent is N',N-dimethylacetamide.

13. The formulation of claim 12 wherein N',N-dimethylacetamide is at a concentration of 5% to 7%.

14. The formulation of claim 11 wherein the water miscible, physiologically acceptable, busulfan solvent is polyethyleneglycol.

15. The formulation of claim 14 wherein polyethyleneglycol is at a concentration of 5% to 50%.

16. The formulation of claim 14 wherein the polyethyleneglycol has a molecular weight between 200 and 2000.

17. The formulation of claim 14 wherein the polyethyleneglycol has a molecular weight between 350 and 450.

18. The formulation of claim 8 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.

19. The formulation of claim 18 wherein the aqueous carrier solution allowing busulfan solubility and stability is a polyethyleneglycol solution.

20. The formulation of claim 8 wherein the water miscible, physiologically acceptable, busulfan solvent is propylene glycol.

21. The formulation of claim 1 wherein the water miscible, physiologically acceptable, busulfan solvent is an aqueous solution of hydroxypropylbetacyclodextrin.

22. A pharmaceutically acceptable formulation for intravascular administration of busulfan comprising about 1-7.5 mg/ml dissolved busulfan, 35-45% polyethyleneglycol-400, water and 5-15% N',N-dimethylacetamide.

23. A pharmaceutically acceptable formulation for intravascular administration of busulfan comprising about 1-10 mg/ml dissolved busulfan, 35-45% polyethyleneglycol-400, water and 15-25% N',N-dimethylacetamide.

24. A method for treating a patient for a malignant condition responsive to busulfan, the method comprising:

obtaining an intravascularly administrable busulfan preparation; and

intravascularly administering said preparation to the patient in an amount effective to treat said condition.

25. The method of claim 24 wherein the malignant condition is a localized solid tumor and the intravascular administration is intraarterial to regionally perfuse said solid tumor.

26. A method for treating leukemia or a lymphoma in a patient undergoing a bone marrow transplant, the method comprising:

obtaining an intravenously administrable busulfan preparation; and

intravenously administering said preparation to the patient having leukemia or a lymphoma in an amount conditioning the patient for the bone marrow transplant.

27. The method of claim 24, or 26 wherein the amount of busulfan administered is from about 0.01 to 1 mg/kg every 6 hours.

28. The method of claim 24, or 26 wherein the preparation is the formulation of claim 15.

29. The method of claim 28 wherein the malignant condition is a breast cancer, leukemia or a lymphoma.

30. The method of claim 29 wherein the leukemia is acute myelogenous leukemia.

31. The method of claim 29 wherein the leukemia is chronic myelogenous leukemia.
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