Gastric retained gabapentin dosage form

• US 8,333,992 B2
• Filed: 07/27/2012
• Issued: 12/18/2012
• Est. Priority Date: 10/25/2001
• Status: Expired due to Term

• Current Assignee: Almatica Pharma LLC (Alvogen Inc.)
• Original Assignee: Depomed Incorporated (Assertio Holdings, Inc.)
• Inventors: Berner, Bret, Hou, Sui Yuen Eddie, Gusler, Gloria M.
• Primary Examiner(s): Wax, Robert A
• Assistant Examiner(s): Tcherkasskaya, Olga V
• Application Number:
  US13/560,938
• Publication Number:
  US 20120289601A1
• Time in Patent Office: 144 Days
• Field of Search: None
• US Class Current: 424/473
• CPC Class Codes: A61K 31/195 having an amino group
• CPC Class Codes: A61K 31/197 the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid carnitine A61K31/205
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0002 Galenical forms characterised by the drug release technique; Application systems commanded by energy
• CPC Class Codes: A61K 9/0065 Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/48 Preparations in capsules, e.g. of gelatin, of chocolate A61K9/0004 takes precedence; bite capsules A61K9/0056
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.

Claims

1. A dosage form, comprising:

a matrix comprising gabapentin, wherein upon ingestion of the dosage form by a human subject gabapentin is released from the matrix into the upper gastrointestinal tract over about 5-12 hours at a rate sufficient to achieve a lower maximum plasma concentration than that provided by an immediate release dosage form comprising an equal amount of gabapentin, and bioavailability of gabapentin is at least 80% of that provided by the immediate release dosage form comprising an equal amount of gabapentin as measured by the area under the plasma concentration-time curve, AUC_inf.

2. The dosage form of claim 1, wherein the time to reach maximum plasma concentration is at least 5.6 hours±

34.9%.

3. The dosage form of claim 1, comprising a dose of gabapentin of between about 300-600 mg.

4. The dosage form of claim 1, wherein the matrix is a polymer matrix.

5. The dosage form of claim 4, wherein the polymer matrix is comprised of a swellable, hydrophilic polymer.

6. The dosage form of claim 5, wherein the gabapentin is released from the polymer matrix by diffusion.

7. The dosage form of claim 1, wherein the gabapentin is released from the matrix at a rate sufficient to achieve a maximum plasma concentration of at least about 3 μ

g/mL.

8. The dosage form of claim 1, wherein the ratio of the maximum plasma concentration to the plasma concentration at 15 hours after administration is no more than about 2.

9. A dosage form, comprising:

a matrix comprising 300 mg or 600 mg gabapentin, wherein upon ingestion by a human subject of one 600 mg dosage form or upon ingestion of two 300 mg dosage forms gabapentin is released from the matrix into the upper gastrointestinal tract over about 5-12 hours at a rate sufficient to achieve a lower maximum plasma concentration than that provided by an immediate release dosage form comprising an equal amount of gabapentin, and bioavailability of gabapentin is at least 80% of that provided by the immediate release dosage form comprising an equal amount of gabapentin as measured by the area under the plasma concentration-time curve, AUC_inf.

10. The dosage form of claim 9, wherein the time to reach maximum plasma concentration is at least 5.6 hours±

34.9%.

11. The dosage form of claim 9, wherein the matrix is a polymer matrix.

12. The dosage form of claim 11, wherein the polymer matrix is comprised of a swellable, hydrophilic polymer.

13. The dosage form of claim 12, wherein the gabapentin is released from the polymer matrix by diffusion.

14. The dosage form of claim 9, wherein the gabapentin is released from the matrix at a rate sufficient to achieve a maximum plasma concentration of at least about 3 μ

g/mL.

15. A method of treating a condition responsive to a therapeutic dose of gabapentin, comprising:

orally administering to a human subject a dosage form comprising a matrix comprising gabapentin, wherein upon ingestion of the dosage form gabapentin is released from the matrix into the upper gastrointestinal tract over about 5-12 hours at a rate sufficient to achieve a lower maximum plasma concentration than that provided by an immediate release dosage form comprising an equal amount of gabapentin, and bioavailability of gabapentin is at least 80% of that provided by the immediate release dosage form comprising an equal amount of gabapentin as measured by the area under the plasma concentration-time curve, AUC_inf.

16. The method of claim 15, wherein the time to reach maximum plasma concentration is at least 5.6 hours±

34.9%.

17. The method of claim 15, wherein the matrix is a polymer matrix.

18. The method of claim 17, wherein the polymer matrix is comprised of a swellable, hydrophilic polymer.

19. The method of claim 15, wherein the condition is pain.

20. The method of claim 15, wherein the condition is neuropathic pain.

21. The method of claim 15, wherein the gabapentin is released from the matrix at a rate sufficient to achieve a maximum plasma concentration of at least about 3 μ

g/mL.

22. A method of treating a condition responsive to a therapeutic dose of gabapentin, comprising:

orally administering to a human subject a dosage form comprising a matrix comprising gabapentin, wherein gabapentin is released from the matrix into the upper gastrointestinal tract over about 5-12 hours at a rate sufficient to achieve a longer time to the maximum plasma concentration than that provided by an immediate release dosage form comprising an equal amount of gabapentin, and bioavailability of gabapentin is at least 80% of that provided by the immediate release dosage form comprising an equal amount of gabapentin as measured by the area under the plasma concentration-time curve, AUC_inf.

23. The method of claim 22, wherein the matrix is a polymer matrix.

24. The method of claim 23, wherein the polymer matrix is comprised of a swellable, hydrophilic polymer.

25. The method of claim 22, wherein the condition is pain.

26. The method of claim 25, wherein the condition is neuropathic pain.

27. The method of claim 22, wherein the gabapentin is released from the matrix at a rate sufficient to achieve a maximum plasma concentration of at least about 3 μ

g/mL.