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Claims for Patent: 9,017,731

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Claims for Patent: 9,017,731

Title:Composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles
Abstract: The invention relates to dosage forms that provide prolonged therapy. In particular, the invention relates to dosage forms including various pluralities of drug-containing resin particles. In a particular embodiment, the drug dosage form comprises a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles. The invention also relates to methods of making these dosage forms and methods of treating using these dosage forms.
Inventor(s): Tengler; Mark (Colleyville, TX), McMahen; Russell (Flower Mound, TX)
Assignee: Neos Therapeutics, LP (Grand Prairie, TX)
Application Number:13/844,537
Patent Claims: 1. A pharmaceutical composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles, wherein 30 to 50% by weight of said amphetamines are present in a first plurality of drug-resin particles that are uncoated and 50 to 70% by weight of said amphetamines are present in a second plurality of drug-resin particles that are coated with a delayed release coating.

2. The composition of claim 1, wherein the second plurality of drug resin particles comprises a triggered-release coating triggered by a pH change.

3. The composition of claim 2, wherein the triggered-release coating is cellulose acetate phthalate, cellulose acetate trimellitate, hydroxypropyl methylcellulose phthalate, polyvinyl acetate phthalate, carboxymethylethylcellulose, co-polymerized methacrylic acid/methacrylic acid methyl esters, co-polymerized methacrylic acid/acrylic acid ethyl esters, or mixtures thereof.

4. The composition of claim 1, wherein the resin particles are strong acidic cation exchange resins, selected from the group consisting of polistirex, polacrilex, cholestyramine, polacrilin or mixtures thereof.

5. The composition of claim 1, wherein 40%-50% by weight of said amphetamines are present in the first plurality of drug-resin particles and 50-60% by weight of said amphetamines are present in the second plurality of drug-resin particles.

6. The composition of claim 5, wherein about 45% by weight of said amphetamines are present in the first plurality of drug-resin particles and about 55% by weight of said amphetamines are present in the second plurality of drug-resin particles.

7. The composition of claim 1, wherein the composition is a liquid suspension, chewable composition, or an orally disintegrating tablet composition.

8. The composition of claim 1, wherein said amphetamines in said drug-resin particles comprise 25% levo-amphetamine and 75% dextro-amphetamine.

9. The composition of claim 1, wherein the amount of said amphetamines is 2-60 mg.

10. The composition of claim 1, wherein 40-45% of said amphetamines is released within the first 45 minutes after the drug-resin particles are introduced into an in vitro dissolution assay, followed by a period of substantially no amphetamine release from 45 minutes to 2 hours, and concluding with period of from 2 to 8 hours during which substantially all of the remainder of said amphetamies is released, wherein the conditions of the dissolution assay are an initial dissolution medium of 0.1 N HCl, and after 2 hours, the medium is adjusted to a pH of about 6.8; and the dissolution assay is performed using a USP Apparatus 2.

11. The composition of claim 1, wherein the delayed release coating releases substantially all of said amphetamines in the second plurality of drug-resin particles within about 60 minutes after initiation of the delayed release.

12. A pharmaceutical composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles, wherein said composition comprises a first plurality of drug-resin particles that are uncoated and a second plurality of drug-resin particles that are coated with a delayed release coating, wherein a mammal receiving said composition, in the presence of ethanol, is exposed to a reduced amount of amphetamines compared to when said mammal receives a composition without resin particles in the presence of ethanol, said composition comprising a mixture of dextroamphetamine sulfate, dextroamphetamine saccharate, amphetamine aspartate, and amphetamine sulfate.

13. The composition of claim 1, wherein the amount of said amphetamines is equivalent to the total amount of dextro- and levo-amphetamines present in a 5 mg, 10 mg, 15 mg, 20 mg, 25 mg, or 30 mg reference composition without resin particles which comprises a mixture of dextroamphetamine sulfate, dextroamphetamine saccharate, amphetamine aspartate, and amphetamine sulfate.

14. A pharmaceutical composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles, wherein said composition comprises a first plurality of drug-resin particles that are uncoated and a second plurality of drug-resin particles that are coated with a delayed release coating, wherein said composition is an orally disintegrating tablet and is effective to provide a mean plasma concentration profile in human ADHD patients which has the following AUC and C.sub.max values for a 30 mg total dose, or respective AUC and C.sub.max values directly proportional thereto for a total dose other than 30 mg: (a) an AUC.sub.0-4 of 85.8 ng hr/mL--20%/+25% and a C.sub.max of 44.5 ng/mL--20%/+25% for dextroamphetamine and/or an AUC.sub.0-4 of 26.3 ng hr/mL--20%/+25% and a C.sub.max of 14.2 ng/mL--20%/+25% for levoamphetamine; (b) an AUC.sub.0-5 of 126.3 ng hr/mL--20%/+25% and a C.sub.max of 44.5 ng/mL--20%/+25% for dextroamphetamine and/or an AUC.sub.0-5 of 39.1 ng hr/mL--20%/+25% and a C.sub.max of 14.2 ng/mL--20%/+25% for levoamphetamine; (c) an AUC.sub.4-12 of 291 ng hr/mL--20%/+25% and a C.sub.max of 44.5 ng/mL--20%/+25% for dextroamphetamine and/or an AUC.sub.4-12 of 95.1 ng hr/mL--20%/+25% and a C.sub.max of 14.2 ng/mL--20%/+25% for levoamphetamine; (d) an AUC.sub.5-12 of 250.5 ng hr/mL--20%/+25% and a C.sub.max of 44.5 ng/mL--20%/+25% for dextroamphetamine and/or an AUC.sub.5-12 of 82.3 ng hr/mL--20%/+25% and a C.sub.max of 14.2 ng/mL--20%/+25% for levoamphetamine; and/or (e) an AUC.sub.0-24 of 613.3 ng hr/mL--20%/+25% and a C.sub.max of 44.5 ng/mL--20%/+25% for dextroamphetamine and/or an AUC.sub.0-24 of 204.9 ng hr/mL--20%/+25% and a C.sub.max of 14.2 ng/mL--20%/+25% for levoamphetamine.

15. A pharmaceutical composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles, wherein said composition comprises a first plurality of drug-resin particles that are uncoated and a second plurality of drug-resin particles that are coated with a delayed release coating, wherein said composition is a liquid suspension and is effective to provide a mean plasma concentration profile in human ADHD patients which has the following AUC and C.sub.max values for a 30 mg total dose, or respective AUC and C.sub.max values directly proportional thereto for a total dose other than 30 mg: (a) an AUC.sub.0-4 of 104.7 ng hr/mL--20%/+25% and a C.sub.max of 46.3 ng/mL--20%/+25% for dextroamphetamine and/or an AUC.sub.0-4 of 31.8 ng hr/mL--20%/+25% and a C.sub.max of 14.6 ng/mL--20%/+25% for levoamphetamine; (b) an AUC.sub.0-5 of 148.6 ng hr/mL--20%/+25% and a C.sub.max of 46.3 ng/mL--20%/+25% for dextroamphetamine and/or an AUC.sub.0-5 of 45.7 ng hr/mL--20%/+25% and a C.sub.max of 14.6 ng/mL--20%/+25% for levoamphetamine; and/or (c) an AUC.sub.4-12 of 300.3 ng hr/mL--20%/+25% and a C.sub.max of 46.3 ng/mL--20%/+25% for dextroamphetamine and/or an AUC.sub.4-12 of 96.8 ng hr/mL--20%/+25% and a C.sub.max of 14.6 ng/mL--20%/+25% for levoamphetamine.

16. A pharmaceutical composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles, wherein said composition comprises a first plurality of drug-resin particles that are uncoated and a second plurality of drug-resin particles that are coated with a delayed release coating, wherein said composition, when containing about a total amphetamine dose of 30 mg, will produce in a human, a mean plasma concentration versus time curve (ng/ml versus hours) having an area under the curve (AUC.sub.0-.infin.) of about 1140 to about 1240 for total amphetamines (dextroamphetamine+levoamphetamine).

17. A pharmaceutical composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles, wherein said composition comprises a first plurality of drug-resin particles that are uncoated and a second plurality of drug-resin particles that are coated with a delayed release coating, wherein one or more in vivo pharmacokinetic parameters of the composition selected from the group consisting of C.sub.max, AUC.sub.0-5, AUC.sub.5-12, AUC.sub.5-24, AUC.sub.5-t, AUC.sub.0-12, AUC.sub.0-24, AUC.sub.0-t, and AUC.sub.0-.infin. have a 90% confidence interval with upper and lower bounds within a range from 90%-115% of the value of the same parameter(s) for a bioequivalent reference composition.

18. A pharmaceutical composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles, wherein said composition comprises a first plurality of drug-resin particles that are uncoated and a second plurality of drug-resin particles that are coated with a delayed release coating, wherein said composition is a liquid suspension and a human receiving said composition substantially contemporaneously with food is exposed to an increased amount of amphetamines in the first 4 hours compared to a human receiving a reference composition without resin particles under similar exposure to food, said reference composition comprising a mixture of dextroamphetamine sulfate, dextroamphetamine saccharate, amphetamine aspartate, and amphetamine sulfate.

19. A pharmaceutical composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles, wherein about 50% by weight of said amphetamines are present in a first plurality of drug-resin particles that are uncoated and about 50% by weight of said amphetamines are present in a second plurality of drug-resin particles that are coated with a delayed release coating.

20. A pharmaceutical composition comprising a mixture of dextro- and levo-amphetamines complexed with ion-exchange resin particles to form drug resin particles, wherein said composition comprises a first plurality of drug-resin particles that are uncoated and a second plurality of drug-resin particles that are coated with a delayed release coating and wherein said composition has an in vivo fasted serum profile with a first and second peak wherein said first peak occurs between 1 and 3 hours after ingestion of the composition and said second peak occurs between 4 and 7 hours after ingestion and is the C.sub.max.
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