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Claims for Patent: 8,563,033

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Claims for Patent: 8,563,033

Title:Orally effective methylphenidate extended release powder and aqueous suspension product
Abstract: An oral methylphenidate powder which is reconstitutable into a final oral aqueous sustained release formulation containing at least about 50%, or at least about 80% by weight water based on the total weight of the suspension, is provided. The powder is a blend containing a combination of an uncoated methylphenidate--ion exchange resin complex, a barrier coated methylphenidate--ion exchange resin complex--matrix, and a water soluble buffering agent such that upon formed into an aqueous liquid formulation, the formulation has a pH in the range of about 3.5 to about 5, or about 4 to about 4.5. Following administration of a single dose of the oral aqueous methylphenidate suspension, a therapeutically effective amount of methylphenidate is reached in less than one hour and the composition provides a twelve-hour extended release profile.
Inventor(s): Mehta; Ketan (Cranbury, NJ), Tu; Yu-Hsing (West Windsor, NJ), Perumal; Ashok (Edison, NJ)
Assignee: Tris Pharma Inc. (Monmouth Junction, NJ)
Application Number:13/905,808
Patent Claims: 1. A methylphenidate aqueous extended release oral suspension comprising (1) an immediate release methylphenidate component, (2) a sustained release methylphenidate component, and (3) water, said suspension having a pH of about 3.5 to about 5, wherein said suspension provides a single mean average plasma concentration peak and a therapeutically effective plasma profile for about 12 hours for methylphenidate, and wherein the suspension has a pharmacokinetic profile in which the single mean plasma concentration peak for methylphenidate has an area under the curve (AUC).sub.0.fwdarw..infin. of about 114 to about 180 ng-hr/mL, C.sub.max of about 11 to about 17 ng/mL, T.sub.max of about 4 to about 5.25 hours, and T.sub.1/2 of about 5 to about 7 hours following a single oral administration of said suspension at a dose equivalent to 60 mg racemic methylphenidate HCl in adults.

2. The suspension according to claim 1, wherein said suspension has a pH in the range of about 4 to about 4.5.

3. The suspension according to claim 1 wherein the pharmacokinetic profile of d-methylphenidate has an AUC.sub.0-.infin. of about 143.65 ng-hr/mL, C.sub.max of about 13.61 ng/mL, T.sub.max of about 5 hours and T.sub.1/2 of about 5.65 hours following a single oral administration of an aqueous suspension at a dose equivalent to 60 mg racemic methylphenidate HCl in adults.

4. The suspension according to claim 1, wherein said suspension contains at least about 80% of water by weight based on the total weight of the suspension.

5. The suspension according to claim 1, wherein said methylphenidate in the immediate release and/or sustained release component is independently selected from the group consisting of racemic methylphenidate and dexmethylphenidate.

6. The suspension according to claim 1, which comprises about 10 to about 30 parts by weight of methylphenidate as provided in the immediate release component and to about 70 to about 90 parts by weight of sustained release methylphenidate, based upon the total weight of methylphenidate in the suspension.

7. The suspension according to claim 1, further comprising a buffering agent selected from the group consisting of one or more of a pharmaceutically acceptable acid consisting of citric acid, ascorbic acid, acetic acid, tartartic acid, phosphoric acid, a pharmaceutically acceptable salt of citric acid, ascorbic acid, acetic acid, tartartic acid, phosphoric acid, or a mixture of said pharmaceutically acceptable acid or salt, and mixtures thereof.

8. The suspension according to claim 7, wherein the buffering agent is a mixture of sodium citrate and anhydrous citric acid.

9. A method for treating a patient having a condition susceptible to treatment with methylphenidate, the method comprising administering to the patient the suspension according to claim 1, wherein said suspension provides a therapeutically effective amount of methylphenidate within 45 minutes after administering of said suspension and a single average plasma concentration peak.

10. The method according to claim 9, wherein the suspension which has a pH from about 4 to about 4.5.

11. A methylphenidate aqueous extended release oral suspension comprising (1) an immediate release methylphenidate component, (2) a sustained release methylphenidate component, and (3) water, said suspension having a pH of about 3.5 to about 5, wherein said suspension provides a single mean average plasma concentration peak and a therapeutically effective plasma profile for about 12 hours for methylphenidate, and wherein the suspension has a pharmacokinetic profile in which the single mean plasma concentration peak for methylphenidate has an area under the curve (AUC).sub.0.sub..fwdarw..sub..infin.of about 137.2 to about 214.4 ng-hr/mL, C.sub.max of about 13.6 to about 21.3 ng/mL, T.sub.max of about 3 to about 5 hours, following a single oral administration of said suspension at a dose equivalent to 72 mg racemic methylphenidate HCl in adults.

12. The suspension according to claim 11 wherein said suspension has a pharmacokinetic profile in which methylphenidate has an AUC.sub.0-.infin. of about 171.5 ng-hr/mL, a C.sub.max of about 17.0 ng/mL, and a T.sub.max of about 3.77 hours following a single oral administration of an aqueous suspension at a dose equivalent to 72 mg racemic methylphenidate HCl in adults.

13. The suspension according to claim 11, wherein said suspension con at least about 80% of water by weight based on the total weight of the suspension.

14. The suspension according to claim 11, wherein said methylphenidate in immediate release and/or sustained release component is independently selected from the group consisting of racemic methylphenidate and dexmethylphenidate.

15. The suspension according to claim 11, which comprises about 10 to about 30 parts by weight of methylphenidate as provided in the immediate release component and to about 70 to about 90 parts by weight of sustained release methylphenidate, based upon the total weight of methylphenidate in the suspension.

16. The suspension according to claim 11, further comprising a buffering agent selected from the group consisting of one or more of a pharmaceutically acceptable acid selected from the group consisting of citric acid, ascorbic acid, acetic acid, tartartic acid, phosphoric acid, a pharmaceutically acceptable salt of citric acid, ascorbic acid, acetic acid, tartartic acid, phosphoric acid, or a mixture of said pharmaceutically acceptable acid or salt, and mixtures thereof.

17. The suspension according to claim 16, wherein the buffering age is a of sodium citrate and anhydrous citric acid.

18. A method for treating a patient having a condition susceptible to treatment with methylphenidate, the method comprising administering to the patient the suspension according to claim 11, wherein said suspension provides a therapeutically effective amount of methylphenidate within 45 minutes after administering of said suspension and a single average plasma concentration peak.

19. The method according to claim 18, wherein the suspension which has a pH from about 4 to about 4.5.
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