Gastric retained gabapentin dosage form

• US 7,731,989 B2
• Filed: 09/26/2008
• Issued: 06/08/2010
• Est. Priority Date: 10/25/2001
• Status: Expired due to Fees

• 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): Sheikh; Humera N
• Application Number:
  US12/239,591
• Publication Number:
  US 20090017121A1
• Time in Patent Office: 620 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 between about 100 mg to about 4800 mg of gabapentin or pharmaceutically acceptable salt thereof, dispersed in a single polymer matrix comprising at least one swellable hydrophilic polymer that swells unrestrained dimensionally by imbibing water to increase its size to promote gastric retention of the dosage form in a stomach in a fed mode, wherein upon contact with water, gabapentin is released by diffusion from the dosage form over a period of at least five hours and at least 40 wt % of the gabapentin is retained in the dosage form 1 hour after administration.

2. The dosage form of claim 1 wherein the dosage form swells to approximately 115% of its volume prior to administration within one hour after administration.

3. The dosage form of claim 1, wherein the dosage form swells to approximately 130% of its volume prior to administration at a time later than one hour after administration.

4. The dosage form of claim 1, comprising between about 200-4000 mg gabapentin.

5. The dosage form of claim 1, comprising between about 200-2700 mg gabapentin.

6. The dosage form of claim 1, comprising between about 300-3600 mg gabapentin.

7. The dosage form of claim 1, comprising between about 500-3600 mg gabapentin.

8. The dosage form of claim 1, comprising between about 900-3600mg gabapentin.

9. The dosage form of claim 1, comprising between about 900-2400 mg gabapentin.

10. The dosage form of claim 1, wherein the gabapentin has a bioavailability greater than or equal to 80% of an equal dose of gabapentin in an immediate release dosage form.

11. The dosage form of claim 1, wherein the polymer matrix is comprised of a polymer having a molecular weight of between about 4×

10³ to 1×

10⁷ Daltons.

12. The dosage form of claim 1, wherein the swellable hydrophilic polymer comprises poly(ethylene oxide).

13. The dosage form of claim 12 wherein the poly(ethylene oxide) has a viscosity average molecular weight of between 2×

10⁶ and 7×

10⁶ Daltons.

14. The dosage form of claim 1, wherein the swellable hydrophilic polymer comprises hydroxypropylmethylcellulose.

15. The dosage form of claim 14, wherein the hydroxypropylmethylcellulose has a molecular weight such that a 1% aqueous solution has a viscosity at room temperature of between about 4,000-10,0000 centipoise.

16. The dosage form of claim 1, wherein the polymer matrix comprises poly(ethylene oxide) and hydroxypropylmethylcellulose.

17. The dosage form of claim 16 further comprising a lubricating agent.

18. The dosage form of claim 17 wherein the lubricating agent is magnesium stearate.

19. The dosage form of claim 1, comprising about 600 mg gabapentin.

20. The dosage form of claim 1, comprising about 300 mg of gabapentin.