Patent EA-001386-B1 (EA)
Title: Compositions, comprising antifungal agent and acetate buffer
Inventor: NERURCAR MANEESH J
IPC: A61K47/12
Filed: 1997-04-15
Abstract: 1. A pharmaceutical composition for intravenous administration to a patient comprising  a) a pharmaceutically effective amount of a compound having the formula    and the pharmaceutically acceptable salts thereof,  b) a pharmaceutically acceptable amount of an excipient such as a bulking sugar or combination of bulking sugars effective to form a lyophilized cake; and  c) a pharmaceutically acceptable amount of an acetate buffer effective to provide a pharmaceutically acceptable Ph 2. A pharmaceutical composition of claim 1 comprising  a) a pharmaceutically effective amount of Compound I; b) between about 10-200 mg/ml of an excipient such as bulking sugar or combination of bulking sugars effective to form a lyophilized cake; and  c) a pharmaceutically acceptable amount of an acetate buffer effective to provide a pH of between about 5 and 7. 3. The composition of claim 2 comprising about 5-200 mg/ml of Compound I or a pharmaceutically acceptable salt thereof, about 12.5 mM to about 200 mM of an acetate buffer, about 10-200 mg/ml of bulking agent, and water. 4. The composition of claim 3 comprising about 30-50 mg/ml of Compound I or a pharmaceutically acceptable salt thereof, about 20-60 mM of an acetate buffer, about 30-70 mg/ml of bulking sugar or combination of bulking sugars effective to form a lyophilized cake, and water. 5. The composition of claim 4 comprising 42 mg/ml of Compound I or a pharmaceutically acceptable salt thereof, 25 mM of an acetate buffer, 30 mg/ml of sucrose, 20 mg/ml of mannitol, and water. 6. The composition of claim 4 comprising 42 mg/ml of Compound I or a pharmaceutically acceptable salt thereof, 50 mM of an acetate buffer, 30 mg/ml of sucrose, 20 mg/ml of mannitol, and water. 7. A method for treating and/or preventing fungal infections in a mammal, comprising intravenously treating the mammal with a pharmaceutically effective amount of the composition of claim 1. 8. The method of claim 7 where the mammal is a human. 9. A method for treating an infection caused by Candida sp. in a patient which comprises administering to said patient an effective amount of the composition of claim 1. 10. A method for treating an infection caused by Candida sp. in a patient which comprises administering to said patient an effective amount of the composition of claim 5. 11. A method for treating an infection caused by Candida sp. in a patient which comprises administering to said patient an effective amount of the composition of claim 6. 12. A method for treating an infection caused by Aspergillus sp. in a patient which comprises administering to said patient an effective amount of the composition of claim 1. 13. A method for treating an infection caused by Aspergillus sp. in a patient which comprises administering to said patient an effective amount of the composition of claim 5. 14. A method for treating an infection caused by Aspergillus sp. in a patient which comprises administering to said patient an effective amount of the composition of claim 6. 15. A method for treating or preventing an infection or condition caused by Pneumocystis carinii in a patient in need of such treatment or prevention which comprises administering to said patient a preventative or therapeutic amount of the composition of claim 1. 16. A method for treating or preventing an infection or condition caused by Pneumoeystis carinii in a patient in need of such treatment or prevention which comprises administering to said patient a preventative or therapeutic amount of the composition of claim 5. 17. A method for treating or preventing an infection or condition caused by Pneumocystis carinii in a patient in need of such treatment or prevention which comprises administering to said patient a preventative or therapeutic amount of the composition of claim 6. 18. A process for making a pharmaceutical composition containing a compound having the formula   and the pharmaceutically acceptable salts thereof, which comprises the steps of  a) dissolving a bulking agent or combination of agents in water; b) adding acetic acid and adjusting the pH to about 3.7; c) adding Compound I and adjusting the pH to about 5 to about 7 with base; d) filtering the solution thus prepared; e) freezing said solution; and  f) freeze drying the frozen solution.