Claims for Patent: 9,757,394

Summary for Patent: 9,757,394

Title:	Spironolactone aqueous formulations
Abstract:	Disclosed herein is a pharmaceutical composition, comprising: (a) spironolactone; (b) a xanthan gum; (c) an anti-foaming agent; (d) a preservative; (f) a dispersing agent; (g) a sweetening agent; (h) a flavoring agent; (i) optionally a buffer to maintain the pH of the pharmaceutical composition within a range described herein; and (j) a sufficient amount of a water vehicle.
Inventor(s):	Pipho; Anthony (Winterville, NC), DeHart; Michael Paul (Winterville, NC)
Assignee:	CMP DEVELOPMENT LLC (Farmville, NC)
Application Number:	15/337,559
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,757,394
Patent Claims:	1. A pharmaceutical composition, comprising: (a) 0.50% w/v of spironolactone; (b) from 0.18% w/v to 0.36% w/v of a xanthan gum; (c) an anti-foaming agent comprised of 0.20% w/v of a simethicone emulsion; (d) a preservative comprised of from 0.025% w/v to 0.050% w/v of sorbic acid and from 0.10% w/v to 0.20% w/v of potassium sorbate; (e) a dispersing agent comprised of from 2.0% w/v to 2.2% w/v glycerin; (f) a sweetening agent comprises 0.14% w/v sodium saccharin and from 0.03% w/v to 0.04% w/v ammonium glycyrrhizinate; (g) a flavoring agent in an amount that ranges from 0.1% w/v to 0.5% w/v; (h) a buffer to maintain the pH of the pharmaceutical composition from 4.5 to 5.5; wherein the buffer is comprised of from 0.17% w/v to 0.24% w/v citric acid and from 0.36% w/v to 0.48% w/v of a citrate salt; and (i) a sufficient amount of a water vehicle. 2. The pharmaceutical composition of claim 1, wherein the viscosity of the composition ranges from 100 cP to 300 cP. 3. The pharmaceutical composition of claim 1, wherein the anti-foaming agent (c) is comprised of 0.20% w/v of a simethicone emulsion; the preservative (d) is comprised of 0.050% w/v of sorbic acid and 0.20% w/v of potassium sorbate; the dispersing agent (e) is comprised of 2.1% w/v to 2.2% w/v glycerin; and wherein the pharmaceutical composition comprises the buffer comprised of 0.20% w/v citric acid and 0.43% w/v sodium citrate. 4. The pharmaceutical composition of claim 3, wherein xanthan gum is present in an amount of 0.25% w/v. 5. The pharmaceutical composition of claim 4, wherein the viscosity of the composition ranges from 130 cP to 170 cP. 6. The pharmaceutical composition of claim 4, wherein the pH of the pharmaceutical composition ranges from 4.8 to 5.2. 7. An enclosed, amber polyethylene terephthalate (PETE) bottle comprising the composition of claim 4. 8. The PETE bottle of claim 7, wherein the volume of said bottle is 4 oz. or 16 oz. 9. A process for preparing the pharmaceutical composition of claim 1, which comprises: (1) mixing the xanthan gum, anti-foaming agent, preservative, a portion of the sweetening agent, and, the buffer, in water in a first container; (2) mixing the spironolactone, the dispersing agent, and the remaining portion of the sweetening agent in a second container; (3) transferring the contents of the second container to the first container followed by mixing the contents of the first container; (4) adding the flavoring agent to the contents of the first container from step (3); (5) adding water to the first container of step (3) and mixing the contents of the first container; and (6) dispensing the contents of the first container from step (5) into an amber polyethylene terephthalate bottle. 10. A pharmaceutical product prepared by the process as claimed in claim 9. 11. A method for the treatment of hypertension in a subject in need thereof, which comprises administering to the subject a therapeutically effective amount of the pharmaceutical composition of claim 1. 12. The method of claim 11, wherein the composition is administered orally or by a nasogastric tube. 13. A method for the treatment of severe heart failure in a subject in need thereof, which comprises administering to the subject a therapeutically effective amount of the pharmaceutical composition of claim 1; wherein the composition is administered orally or by a nasogastric tube. 14. A pharmaceutical composition comprising: (a) 0.50% w/v spironolactone; (b) 0.25% w/v of a xanthan gum; (c) 0.20% w/v of a simethicone emulsion; (d) a preservative comprised of 0.050% w/v of sorbic acid and 0.20% w/v of potassium sorbate; (e) from 2.1% w/v to 2.2% w/v glycerin; (f) a sweetening agent containing 0.14% w/v sodium saccharin and from 0.03% w/v to 0.04% w/v ammonium glycyrrhizinate; (g) 0.30% w/v of a fruit flavoring agent; (h) a buffer comprised of 0.20% w/v citric acid and 0.43% w/v sodium citrate; and (i) a sufficient amount of a water vehicle. 15. The pharmaceutical composition of claim 14, said composition having a pH of from 4.5 to 5.5. 16. The pharmaceutical composition of claim 14, said composition having a pH of from 4.8 to 5.2. 17. The pharmaceutical composition of claim 14, said composition having a viscosity that ranges from 100 cP to 300 cP. 18. The pharmaceutical composition of claim 14, said composition having a viscosity that ranges from 130 cP to 170 cP. 19. An enclosed, amber polyethylene terephthalate (PETE) bottle having a volume of 4 oz or 16 oz comprising the composition of claim 14. 20. A method for the treatment of hypertension in a subject in need thereof, which comprises administering to the subject a therapeutically effective amount of the pharmaceutical composition of claim 14. 21. The method of claim 14, wherein the composition is administered orally or by a nasogastric tube. 22. A method for the treatment of severe heart failure in a subject in need thereof, which comprises administering to the subject a therapeutically effective amount of the pharmaceutical composition of claim 14; wherein the composition is administered orally or by a nasogastric tube. 23. A method for the treatment of a patient suffering from a skin disorder, which comprises administering to the subject a therapeutically effective amount of the pharmaceutical composition of claim 14, wherein said skin disorder is selected from the group consisting of acne, hirsutism, androgenic alopecia, rosacea, and combinations thereof. 24. The pharmaceutical composition of claim 1, wherein the spironolactone content is 100.+-.10% of labeled content when stored under 40.degree. C. and not more than 25% relative humidity for 6-months. 25. The pharmaceutical composition of claim 14, wherein the spironolactone content is 100.+-.10% labeled content when stored under 40.degree. C. and not more than 25% relative humidity for 6-months. 26. The pharmaceutical composition of claim 1, wherein the spironolactone content is 100.+-.10% of labeled content when stored under 25.degree. C. and 40% relative humidity for 24-months. 27. The pharmaceutical composition of claim 14, wherein the spironolactone content is 100.+-.10% of labeled content when stored under 25.degree. C. and 40% relative humidity for 24-months.