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Claims for Patent: 9,040,083

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Claims for Patent: 9,040,083

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 (Princeton, NJ), Tu; Yu-Hsing (West Windsor, NJ), Perumal; Ashok (Monmouth Junction, NJ)
Assignee: TRIS PHARMA, INC (Monmouth Junction, NJ)
Application Number:14/554,123
Patent Claims: 1. A powder which when admixed with water forms an aqueous oral suspension, said powder comprising (i) an immediate release methylphenidate component, (ii) a sustained release water-insoluble, water-permeable, pH-independent, barrier coated methylphenidate-ion exchange resin complex, and (iii) a buffering agent which adjusts the pH of the oral aqueous suspension comprising the powder to a pH of about 4.2, wherein the oral aqueous suspension provides a pharmacokinetic profile in which d-methylphenidate has an area under the curve (AUC).sub.0-.infin. of about 114 ng-hr/mL to about 180 ng-hr/mL and a C.sub.max of about 11 ng/mL to about 17 ng/mL following a single oral administration of the oral aqueous suspension to adult subjects under fasted conditions at a dose equivalent to 60 mg racemic methylphenidate HCl.

2. The powder according to claim 1, wherein the suspension which comprises the powder further comprises at least about 80% of water based on the total weight of the suspension.

3. The powder according to claim 2, wherein the suspension has less than about 5% loss in potency over a period of about 1 month of storage at room temperature.

4. The powder according to claim 2, wherein the suspension has less than about 1% of an impurity which is threo-.alpha.-phenyl-2-piperidineacetic acid hydrochloride after a period of about 1 month of storage at room temperature.

5. The powder according to claim 2, wherein the suspension has less than about 5% loss in potency over a period of about 4 months of storage at room temperature.

6. The powder according to claim 2, wherein the suspension has less than about 1% of an impurity which is threo-.alpha.-phenyl-2-piperidineacetic acid hydrochloride after a period of about 4 months of storage at room temperature.

7. The powder according to claim 1, wherein the methylphenidate in the immediate release methylphenidate component of (i) comprises about 20% w/w of the total methylphenidate in said powder.

8. The powder according to claim 1, wherein the immediate release methylphenidate component comprises an uncoated methylphenidate-ion exchange resin complex.

9. The powder according to claim 1, wherein the immediate release methylphenidate component comprises a methylphenidate-ion exchange resin complex having a coating that provides immediate release.

10. The powder according to claim 1, wherein the barrier coating of the sustained release water-insoluble, water-permeable, pH-independent, barrier coated methylphenidate-ion exchange resin complex comprises a polyvinylacetate polymer and a plasticizer.

11. The powder according to claim 10, wherein the barrier coating is cured.

12. The powder according to claim 1, wherein the barrier coating of the sustained release water-insoluble, water-permeable, pH-independent, barrier coated methylphenidate-ion exchange resin complex comprises ethylcellulose.

13. The powder according to claim 1, wherein the barrier coating of the sustained release water-insoluble, water-permeable, pH-independent, barrier coated methylphenidate-ion exchange resin complex comprises a methyl methyacrylate polymer or co-polymer.

14. The powder according to claim 1, which provides the aqueous oral suspension comprising at least about 70% of water based on the total weight of the suspension.

15. The powder according to claim 1, wherein the oral aqueous suspension has a therapeutically effective plasma profile for methylphenidate of about 12 hours following a single oral administration of the oral aqueous suspension to adult subjects under fasted conditions at a dose equivalent to 60 mg racemic methylphenidate HCl.

16. The powder according to claim 1, wherein the oral aqueous suspension provides a therapeutically effective amount of methylphenidate within 45 minutes after a single oral administration of the oral aqueous suspension to adult subjects under fasted conditions at a dose equivalent to 60 mg racemic methylphenidate HCl.

17. The powder according to claim 1, wherein the oral aqueous suspension provides a single average plasma concentration peak following a single oral administration of the oral aqueous suspension to adult subjects under fasting conditions at a dose equivalent to 60 mg racemic methylphenidate HCl.

18. The powder according to claim 1, wherein the oral aqueous suspension provides a T.sub.max of about 4 hours to about 5.25 hours following a single oral administration of the oral aqueous suspension to adult subjects under fasted conditions at a dose equivalent to 60 mg racemic methylphenidate HCl.

19. The powder according to claim 1, wherein following a single oral administration of the oral aqueous suspension to adult subjects at a dose equivalent to 60 mg racemic methylphenidate HCl said suspension provides a reduced T.sub.max for d-methylphenidate in adult subjects fed with a high-fat meal prior to administration compared to adult subjects in a fasted state prior to administration.

20. The powder according to claim 19, wherein following a single oral administration of the oral aqueous suspension at a dose equivalent to 60 mg racemic methylphenidate HCl, the oral aqueous suspension provides a T.sub.max for d-methylphenidate reduced by about 60 minutes in adult subjects fed with a high-fat meal prior to administration compared to adult subjects in a fasted state prior to administration.

21. A powder which when admixed with water forms an aqueous oral suspension, said powder comprising (i) an immediate release methylphenidate component, (ii) a sustained release water-insoluble, water-permeable, pH-independent, barrier coated methylphenidate-ion exchange resin complex, and (iii) a buffering agent which adjusts the pH of the oral aqueous suspension comprising the powder to a pH of about 4.2, wherein the oral aqueous suspension comprising the powder further comprises at least about 80% of water based on the total weight of the suspension, wherein the oral aqueous suspension has less than about 1% of threo-.alpha.-phenyl-2-piperidineacetic acid hydrochloride impurity after a period of about 1 month of storage at room temperature, and wherein following a single oral administration of the aqueous oral suspension to adult subjects under fasted conditions, at a dose equivalent to 60 mg racemic methylphenidate HCl, the oral aqueous suspension has a pharmacokinetic profile in which d-methylphenidate has an area under the curve (AUC).sub.0-.infin. of about 114 ng-hr/mL to about 180 ng-hr/mL in adults under fasted conditions, a C.sub.max of about 11 ng/mL to about 17 ng/mL in adults, and wherein following a single administration of the aqueous oral suspension to adult, the d-methylphenidate has a reduced T.sub.max in adults subjects fed with a high-fat meal prior to administration compared to adult subjects in a fasted state prior to administration.

22. The powder according to claim 21, wherein following a single oral administration of an aqueous oral suspension at a dose equivalent to 60 mg racemic methylphenidate HCl the oral aqueous suspension has a pharmacokinetic profile in which the d-methylphenidate has a T.sub.max reduced by about 60 minutes in adults subjects fed with a high-fat meal prior to administration compared to adult subjects in a fasted state prior to administration.
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