Claims for Patent: 11,040,023

Summary for Patent: 11,040,023

Title:	Enalapril formulations
Abstract:	Provided herein are stable enalapril oral liquid formulations. Also provided herein are methods of using enalapril oral liquid formulations for the treatment of certain diseases including hypertension, heart failure and asymptomatic left ventricular dysfunction.
Inventor(s):	Gerold L. Mosher, David W. Miles
Assignee:	Azurity Pharmaceuticals Inc
Application Number:	US17/150,587
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,040,023
Patent Claims:	1. A stable oral liquid formulation, consisting essentially of: (i) about 0.6 to about 1.2 mg/ml enalapril or a pharmaceutically acceptable salt or solvate thereof; (ii) a sweetener; (iii) a preservative, wherein the preservative comprises sodium benzoate, a paraben or a mixture of parabens; (iv) water; and (v) optionally a flavoring agent; wherein the formulation is stable at about 5±3° C. for at least 12 months; and wherein the stable oral liquid formulation has about 95% w/w or greater of the initial enalapril amount and about 5% w/w or less total impurity or related substances at the end of the given storage period. 2. The stable oral liquid formulation of claim 1, wherein the formulation is stable at about 5±3° C. for at least 18 months. 3. The stable oral liquid formulation of claim 1, wherein the formulation is stable at about 5±3° C. for at least 24 months. 4. The stable oral liquid formulation of claim 1, wherein the formulation maintains a pH between about 3 and about 4 for at least 3 months at about 5±3° C. 5. The stable oral liquid formulation of claim 1, wherein the formulation maintains a pH between about 3 and about 4 for at least 12 months at about 5±3° C. 6. The stable oral liquid formulation of claim 1, wherein the sweetener is sucralose. 7. The stable oral liquid formulation of claim 6, wherein the sucralose is present in about 0.5 mg/ml to about 0.9 mg/ml in the oral liquid formulation. 8. The stable oral liquid formulation of claim 1, wherein the sweetener is saccharin or a salt thereof. 9. The stable oral liquid formulation of claim 8, wherein the saccharin or a salt thereof is present at about 2 mg/ml in the oral liquid formulation. 10. The stable oral liquid formulation of claim 1, comprising a flavoring agent. 11. The stable oral liquid formulation of claim 1, wherein the enalapril or a pharmaceutically acceptable salt or solvate thereof functions as a buffer. 12. The stable oral liquid formulation of claim 1, wherein the enalapril or a pharmaceutically acceptable salt or solvate thereof is present at about 1.0 mg/ml in the oral liquid formulation. 13. The stable oral liquid formulation of claim 1, wherein the preservative is a mixture of parabens. 14. The stable oral liquid formulation of claim 1, wherein the paraben or the mixture of parabens is methylparaben, ethylparaben, propylparaben, butylparaben, salts thereof, or a combination thereof. 15. The stable oral liquid formulation of claim 1, wherein the mixture of parabens comprises methylparaben and propylparaben. 16. The stable oral liquid formulation of claim 1, wherein the paraben or the mixture of parabens is present at about 0.1 mg/ml to about 2 mg/ml in the oral liquid formulation. 17. The stable oral liquid formulation of claim 1, wherein the preservative comprises sodium benzoate. 18. The stable oral liquid formulation of claim 17, wherein the sodium benzoate is present at about 0.2 mg/ml to about 1.2 mg/ml in the oral liquid formulation. 19. The stable oral liquid formulation of claim 1, consisting essentially of: (i) about 1.0 mg/ml enalapril or a pharmaceutically acceptable salt or solvate thereof; (ii) a sweetener that is sucralose or sodium saccharin; (iii) a preservative, wherein the preservative comprises a mixture of parabens that is present at about 0.1 mg/ml to about 2 mg/ml in the oral liquid formulation; (iv) water; and (v) optionally a flavoring agent. 20. The stable oral liquid formulation of claim 1, consisting essentially of: (i) about 1.0 mg/ml enalapril or a pharmaceutically acceptable salt or solvate thereof; (ii) a sweetener that is sucralose or sodium saccharin; (iii) a preservative, wherein the preservative comprises sodium benzoate that is present at about 0.2 mg/ml to about 1.2 mg/ml in the oral liquid formulation; (iv) water; and (v) optionally a flavoring agent.