LISINOPRIL FORMULATIONS
First Claim
Patent Images
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;
wherein when the preservative is a paraben, the sweetener is not xylitol or mannitol; and
wherein the formulation is stable at about 25±
5°
C. for at least 6 months.
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Accused Products
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.
13 Citations
20 Claims
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1. A stable oral liquid formulation, comprising:
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(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; wherein when the preservative is a paraben, the sweetener is not xylitol or mannitol; and wherein the formulation is stable at about 25±
5°
C. for at least 6 months. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
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19. A stable oral liquid formulation, comprising:
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(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°
C. for at least 12 months.
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20. A stable oral liquid formulation, comprising:
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(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°
C. for at least 12 months.
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Specification