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Last Updated: April 19, 2024

Claims for Patent: 8,703,156


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Summary for Patent: 8,703,156
Title:Liquid formulation for deferiprone with palatable taste
Abstract: An oral pharmaceutical liquid formulation comprising deferiprone and a taste masking composition, said taste masking composition comprising an effective amount of a sweetener (such as sucralose) per liter of liquid composition, an effective amount of a thickening and suspension aid, (for example hydroxyethylcellulose), per liter of liquid composition, an effective amount of a humectant (such as glycerin) per liter of liquid composition, and an effective amount of at least one flavoring agent, wherein a final form of said taste-masked pharmaceutical has a substantially non-bitter and palatable taste.
Inventor(s): Spino; Michael (Pickering, CA), Hui; Anita (Unionville, CA), Yang; Cihua (Richmond Hill, CA), Kabir; Mohammed N. (Richmond Hill, CA)
Assignee: Apotex Technologies Inc. (Toronto, Ontario, CA)
Application Number:12/989,127
Patent Claims: 1. An oral pharmaceutical liquid formulation comprising deferiprone in a concentration of from about 20 grams to about 200 grams per liter of liquid formulation and a taste masking composition, said taste masking composition comprising: a sweetener selected from the group consisting of aspartame, saccharin, saccharin sodium, sucralose and mixtures thereof, in a concentration of about 0.1 grams to about 400 grams per liter of liquid formulation; hydroxyethylcellulose as a thickening and suspension aid, in a concentration of from about 0.5 grams to about 3.0 grams per liter of liquid formulation; glycerin as a humectant in an amount of about 100 grams to about 900 grams per liter of liquid formulation; and at least one flavoring agent selected from the group consisting of natural flavors, natural fruit flavors, artificial flavors, artificial fruit flavors, peppermint, peppermint oils and mixtures thereof; wherein the remainder of the liquid formulation is purified water.

2. The formulation of claim 1 further comprising more than one flavoring agent.

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

4. The formulation of claim 1, wherein said liquid pharmaceutical formulation has a pH from about 2.5 to about 5.0.

5. The formulation of claim 1, wherein the amount of glycerin is about 500 grams per liter of the formulation.

6. The formulation of claim 1, wherein the amount of hydroxyethylcellulose is about 1.0 grams per liter of the formulation.

7. The formulation of claim 4, further comprising concentrated hydrochloric acid.

8. The formulation of claim 1, wherein the sweetening agent is selected from the group consisting of an artificial sweetener selected from the group consisting of aspartame, sucralose and saccharin.

9. The formulation of claim 1, wherein said sweetening agent is present at about 0.1 to about 3 percent by weight of the formulation.

10. The formulation of claim 1, wherein deferiprone is present in an amount of about 50 grams to about 200 grams per liter of the formulation.

11. The formulation of claim 1 wherein the flavoring agent further comprises artificial cherry flavor.

12. The formulation of claim 11 wherein peppermint oil is added as an additional flavor.

13. A liquid pharmaceutical formulation comprising: about 50 to about 200 grams of deferiprone per liter of the formulation, about 15 grams of sucralose per liter of the formulation, about 500 grams of glycerin per liter of the formulation, about 1 gram of hydroxyethylcellulose per liter of the formulation, about 59 grams of concentrated hydrochloric acid per liter of the formulation, about 0.40 grams of FD&C Yellow No. 6 per liter of the formulation, about 2 grams of artificial cherry flavour per liter of the formulation, about 0.10 grams of peppermint oil per liter of the formulation and a sufficient amount of purified water to yield 1 liter of the formulation.

14. The formulation of claim 1, wherein the flavoring agent is selected from the group consisting of cherry, grape, strawberry, orange-blood, melon, banana, and citrus vanilla, and mixtures thereof.

15. The formulation of claim 1, wherein the sweetener is present in an amount of from about 5 grams to about 30 grams per liter of the formulation.

16. The formulation of claim 15, wherein the sweetener is sucralose.

17. A method of treating a patient with iron overloading in a heart, a mitochondria, or a central nervous system including brain, comprising administering to the patient orally the liquid formulation of claim 1.

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