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Last Updated: September 18, 2020

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Claims for Patent: 9,669,008

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Summary for Patent: 9,669,008
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): Mosher; Gerold L. (Kansas City, MO), Miles; David W. (Kansas City, MO)
Assignee: Silvergate Pharmaceuticals, Inc. (Greenwood Village, CO)
Application Number:15/081,603
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,669,008
Patent Claims: 1. A stable oral liquid formulation, comprising: (i) about 1 mg/ml enalapril maleate; (ii) a buffer comprising about 1.82 mg/ml citric acid and about 0.15 mg/mL sodium citrate dihydrate; (iii) about 1 mg/ml of a preservative that is sodium benzoate; and (iv) water; wherein the pH of the formulation is less than about 3.5; and wherein the formulation is stable at about 5.+-.3.degree. C. for at least 12 months; wherein the stable oral liquid formulation has about 95% or greater of the initial enalapril amount and about 5% w/w or less total impurities or related substances at the end of the given storage period.

2. The formulation of claim 1, further comprising a flavoring agent.

3. The formulation of claim 1, wherein the pH is between about 3 and about 3.5.

4. The formulation of claim 3, wherein the pH is about 3.3.

5. The formulation of claim 1, wherein the citrate concentration in the buffer is about 5 mM to about 20 mM.

6. The formulation of claim 5, wherein the citrate concentration in the buffer is about 10 mM.

7. The formulation of claim 1, wherein the formulation is stable at about 5.+-.3.degree. C. for at least 18 months.

8. The formulation of claim 1, wherein the formulation is stable at about 5.+-.3.degree. C. for at least 24 months.

9. The formulation of claim 1, wherein the formulation does not contain mannitol.

10. The formulation of claim 1, wherein the formulation does not contain silicon dioxide.

11. A stable oral liquid formulation, comprising: (i) about 19.3% (w/w of solids) enalapril maleate; (ii) a buffer comprising about 35.2% (w/w of solids) citric acid and about 2.9% (w/w of solids) sodium citrate dihydrate; (iii) about 19.3% (w/w of solids) of a preservative that is sodium benzoate; and (iv) water; wherein the pH of the formulation is less than about 3.5; and wherein the formulation is stable at about 5.+-.3.degree. C. for at least 12 months; wherein the stable oral liquid formulation has about 95% or greater of the initial enalapril amount and about 5% w/w or less total impurities or related substances at the end of the given storage period.

12. The formulation of claim 11, further comprising a flavoring agent.

13. The formulation of claim 11, wherein the pH is between about 3 and about 3.5.

14. The formulation of claim 13, wherein the pH is about 3.3.

15. The formulation of claim 11, wherein the citrate concentration in the buffer is about 5 mM to about 20 mM.

16. The formulation of claim 15, wherein the citrate concentration in the buffer is about 10 mM.

17. The formulation of claim 11, wherein the formulation is stable at about 5.+-.3.degree. C. for at least 24 months.

18. A stable oral liquid formulation, consisting essentially of: (i) about 1 mg/ml enalapril maleate; (ii) about 0.70 mg/ml of a sweetener that is sucralose; (iii) a buffer comprising about 1.82 mg/ml citric acid and about 0.15 mg/ml sodium citrate dihydrate; (iv) about 1 mg/ml of a preservative that is sodium benzoate; (v) a flavoring agent; and (vi) water; wherein the pH of the formulation is less than about 3.5 adjusted by sodium hydroxide or hydrochloric acid if needed; and wherein the formulation is stable at about 5.+-.3.degree. C. for at least 12 months; wherein the stable oral liquid formulation has about 95% or greater of the initial enalapril amount and about 5% w/w or less total impurities or related substances at the end of the given storage period.

19. The stable oral liquid formulation of claim 1, further comprising about 0.70 mg/ml of a sweetener that is sucralose.

20. The stable oral liquid formulation of claim 11, further comprising about 13.5% (w/w of solids) of a sweetener that is sucralose.

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