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Last Updated: November 25, 2020

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Claims for Patent: 9,814,751

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Summary for Patent: 9,814,751
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:15/483,691
Patent Claims: 1. 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 formulation of claim 1, wherein the lisinopril is lisinopril dihydrate.

3. The formulation of claim 1, wherein the pH is between about 4 and about 5.2.

4. The formulation of claim 1, wherein the pH is about 4.9.

5. The formulation of claim 1, wherein the pH is about 5.2.

6. The formulation of claim 1, wherein the formulation is stable at about 25.+-.5.degree. C. for at least 12 months.

7. The formulation of claim 1, wherein the formulation is stable at about 25.+-.5.degree. C. for at least 18 months.

8. The formulation of claim 1, wherein the formulation is stable at about 25.+-.5.degree. C. for at least 24 months.

9. The formulation of claim 1, wherein the buffer concentration is from about 5 to about 50 mM.

10. The formulation of claim 1, wherein the buffer concentration is about 10 mM.

11. The formulation of claim 1, wherein the sweetener is xylitol.

12. The formulation of claim 11, wherein the amount of xylitol is about 140 to about 160 mg/ml.

13. The formulation of claim 1, wherein the sweetener is sucralose.

14. The formulation of claim 13, wherein the amount of sweetener is about 0.5 to about 3 mg/ml.

15. The formulation of claim 1, wherein the preservative is sodium benzoate.

16. The formulation of claim 1, wherein the amount of the preservative is about 0.5 to about 1.2 mg/ml.

17. The formulation of claim 1, wherein the preservative is methylparaben or propylparaben or salts thereof.

18. The formulation of claim 17, wherein the amount of the paraben is about 0.1 to about 2 mg/ml.

19. A stable oral liquid formulation, comprising: (i) about 0.8 to about 1.2 mg/ml lisinopril or a pharmaceutically acceptable salt or solvate thereof; (ii) about 140 to about 160 mg/ml xylitol; (iii) a buffer comprising about 0.5 to about 1.2 mg/ml citric acid and about 1.2 to about 1.7 mg/ml sodium citrate; (iv) about 0.5 to about 1.2 mg/ml sodium benzoate; and (v) water; wherein the pH of the formulation is between about 4 and about 5, and wherein the formulation is stable at about 25.+-.5.degree. C. for at least 12 months.

20. A stable oral liquid formulation, comprising: (i) about 0.5 to about 1% (w/w of solids) lisinopril or a pharmaceutically acceptable salt or solvate thereof; (ii) about 95 to about 98% (w/w of solids) of a sweetener that is xylitol; (iii) a buffer comprising about 0.3 to about 0.7% (w/w of solids) citric acid and about 0.7 to about 1.3% (w/w of solids) sodium citrate; (iv) about 0.4 to about 1.2% (w/w of solids) of a preservative that is sodium benzoate; and (v) water; wherein the pH of the formulation is between about 4 and about 5; and wherein the formulation is stable at about 25.+-.5.degree. C. for at least 12 months.

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