Claims for Patent: 4,448,774

Summary for Patent: 4,448,774

Title:	Steroid formulation
Abstract:	There is described an aqueous pharmaceutical solution comprising a steroid selected from prednisolone, prednisolone sodium phosphate, prednisone and methyl prednisolone, the steroid being present at a concentration of at least 0.3 mg/ml., the pH of the formulation between 5 and 8 and the formulation containing a pharmaceutically acceptable preservative, a pharmaceutically acceptable chelating agent, and being substantially free of ethanol. There is also described a method of treatment of a variety of conditions, particularly in children, using the solution.
Inventor(s):	Clemente; Emmett (Manchester, MA), Fung; Ho-Leung (Getzville, NY), Brousseau; Denise (Andover, MA)
Assignee:	Fisons Corporation (Bedford, MA)
Application Number:	06/452,294
Patent Claims:	1. An aqueous pharmaceutical solution suitable for oral administration comprising as an active ingredient a steroid selected from the group consisting of prednisolone, prednisolone sodium phosphate, prednisone and methyl prednisolone, the steroid being present at a concentration of at least 0.3 mg/ml, the pH of the formulation being between 5 and 8 and the formulation containing a pharmaceutically acceptable preservative, a pharmaceutically acceptable chelating agent, and being substantially free of ethanol. 2. A solution according to claim 1 containing from 0.5 to 5 mg/ml of steroid. 3. A solution according to claim 2 containing from 0.7 to 2 mg/ml of steroid. 4. A solution according to claim 1 containing a sugar. 5. A solution according to claim 4 containing sorbitol or sucrose. 6. A solution according to claim 5 containing from 10 to 50% w/w of sugar. 7. A solution according to claim 6 containing from 25 to 45% w/w/ of the sugar. 8. A solution according to claim 1 containing methyl-hydroxybenzoate. 9. A solution according to claim 8 containing from 0.01 to 0.08% w/w of methyl-hydroxybenzoate. 10. A solution according to claim 1 having a pH in the range 6.5 to 7.5. 11. A solution according to claim 1 containing ethylene diamine tetraacetic acid or a salt thereof. 12. A solution according to claim 11 containing from 0.01 to 0.1% w/w of a salt of ethylene diamine tetraacetic acid. 13. A solution according to claim 12 containing from 0.02 to 0.05% w/w of the disodium salt of ethylene diamine tetraacetic acid. 14. A solution according to claim 1 containing a phosphate buffer. 15. A solution according to claim 1 containing prednisolone sodium phosphate in an amount of from 0.7 to 2 mg/ml, methyl-hydroxybenzoate in an amount of from 0.01 to 0.08% w/w, the disodium salt of ethylene diamine tetraacetic acid in an amount of from 0.02 to 0.05% w/w and sorbitol in an amount of from 25 to 45% w/w. 16. A method of treatment of a patient suffering from an endocrine disorder, a rheumatic disorder, a collagen disease, a dermatologic disease, an allergic state, an ophthalmic disease, a respiratory disease, a haematologic disorder, a neoplastic disease, an edematous state, a gastrointestinal disease or a nervous disease, which conprises administration of an effective amount of a solution according to claim 1 to the patient. 17. A method according to claim 16 wherein the patient is a child and from 5 to 60 ml of the solution is administered per 18. A method according to claim 16 wherein the biological half life of the solution is from 12 to 24 hours. 19. A solution according to claim 1 containing aspartame as a sweetening agent. 20. An aqueous pharmaceutical solution suitable for oral administration to a patient comprising: (a) as an active ingredient a steroid selected from the group consisting of prednisolone, prednisolone sodium phosphate, prednisone and methyl prednisolone; (b) methyl-hydroxybenzoate as a perservative in an amount of from about 0.01 to 0.08% w/w; (c) ethylene diamine tetraacetic acid or a pharmaceutically acceptable salt thereof as a chelating agent in an amount of from about 0.01 to 0.2% w/w; (d) sorbitol or sucrose as a sweetening agent in an amount of from about 10 to 50% w/w; and (e) a phosphate buffer, the pH of the formulation being between about 6.5 and 7.5 and the solution being substantially free of ethanol.