Claims for Patent: 10,039,800

Summary for Patent: 10,039,800

Title:	Lisinopril formulations
Abstract:	Provided herein are stable lisinopril oral liquid formulations. Also provided herein are methods of using lisinopril oral liquid formulations for the treatment of certain diseases including hypertension, heart failure and acute myocardial infarction.
Inventor(s):	Mosher; Gerold L. (Kansas City, MO), Miles; David W. (Kansas City, MO)
Assignee:	SILVERGATE PHARMACEUTICALS, INC. (Greenwood Village, CO)
Application Number:	15/805,934
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,039,800
Patent Claims:	1. A method of treating hypertension in a subject comprising administering to that subject a therapeutically effective amount of a stable oral liquid formulation, comprising: (i) about 1 mg/ml lisinopril or a pharmaceutically acceptable salt or solvate thereof; (ii) a sweetener selected from the group consisting of xylitol, mannitol, sucralose, saccharin, and pharmaceutically acceptable salts thereof; (iii) a buffer comprising citric acid and sodium citrate; (iv) a preservative selected from the group consisting of sodium benzoate, benzoic acid, sorbic acid, methylparaben, propylparaben, and pharmaceutically acceptable salts thereof; and (v) water; provided that when the preservative is a paraben, then the sweetener is not xylitol or mannitol; and wherein the formulation is stable at about 25.+-.5.degree. C. for at least 6 months. 2. The method of claim 1, wherein lisinopril is lisinopril dihydrate. 3. The method of claim 1, wherein the pH is about 4.9. 4. The method of claim 1, wherein the formulation is stable at about 25.+-.5.degree. C. for at least 24 months. 5. The method of claim 1, wherein the hypertension is primary (essential) hypertension. 6. The method of claim 1, wherein the hypertension is secondary hypertension. 7. The method of claim 1, wherein the subject has blood pressure values greater than or equal to 140/90 mm Hg. 8. The method of claim 1, wherein the subject is elderly. 9. The method of claim 1, wherein the subject is a child. 10. The method of claim 1, wherein the formulation is further administered in combination with an agent selected from the group consisting of diuretics, beta blockers, alpha blockers, mixed alpha and beta blockers, calcium channel blockers, angiotensin II receptor antagonists, ACE inhibitors, aldosterone antagonists, and alpha-2 agonists. 11. A method of treating heart failure in a subject comprising administering to that subject a therapeutically effective amount of a stable oral liquid formulation, comprising: (i) about 1 mg/ml lisinopril or a pharmaceutically acceptable salt or solvate thereof; (ii) a sweetener selected from the group consisting of xylitol, mannitol, sucralose, saccharin, and pharmaceutically acceptable salts thereof; (iii) a buffer comprising citric acid and sodium citrate; (iv) a preservative selected from the group consisting of sodium benzoate, benzoic acid, sorbic acid, methylparaben, propylparaben, and pharmaceutically acceptable salts thereof; and (v) water; provided that when the preservative is a paraben, then the sweetener is not xylitol or mannitol; and wherein the formulation is stable at about 25.+-.5.degree. C. for at least 6 months. 12. The method of claim 11, wherein lisinopril is lisinopril dihydrate. 13. The method of claim 11, wherein the pH is about 4.9. 14. The method of claim 11, wherein the formulation is stable at about 25.+-.5.degree. C. for at least 24 months. 15. The method of claim 11, wherein the subject is not responding adequately to diuretics and digitalis. 16. A method of treating a hemodynamically stable subject within 24 hours of acute myocardial infarction comprising administering to that subject a therapeutically effective amount of a stable oral liquid formulation, comprising: (i) about 1 mg/ml lisinopril or a pharmaceutically acceptable salt or solvate thereof; (ii) a sweetener selected from the group consisting of xylitol, mannitol, sucralose, saccharin, and pharmaceutically acceptable salts thereof; (iii) a buffer comprising citric acid and sodium citrate; (iv) a preservative selected from the group consisting of sodium benzoate, benzoic acid, sorbic acid, methylparaben, propylparaben, and pharmaceutically acceptable salts thereof; and (v) water; provided that when the preservative is a paraben, then the sweetener is not xylitol or mannitol; and wherein the formulation is stable at about 25.+-.5.degree. C. for at least 6 months. 17. The method of claim 16, wherein lisinopril is lisinopril dihydrate. 18. The method of claim 16, wherein the pH is about 4.9. 19. The method of claim 16, wherein the formulation is stable at about 25.+-.5.degree. C. for at least 24 months. 20. The method of claim 16, wherein the formulation is further administered in combination with an agent selected from the group consisting of beta blockers, aspirin, and thrombolytics.