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Gastric retentive gabapentin dosage forms and methods for using same

a technology of gastric retentive gabapentin and dosage form, which is applied in the direction of biocide, coating, peptide/protein ingredients, etc., can solve the problems of slowing down the peak plasma level rise, and achieve no side effects, no increase in efficacy, and increased bioavailability

Inactive Publication Date: 2009-07-09
DEPOMED SYST INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention provides a gastric retentive dosage form of gabapentin that overcomes the compliance, bioavailability, and side effect issues associated with conventional immediate release dosage forms. The gastric retentive dosage form requires only once or twice daily dosing, improving patient compliance. It also allows for better absorption, higher bioavailability, and reduced side effects. The gastric retentive dosage form can be used for the treatment of various disease states or conditions that may be treated with conventional immediate release gabapentin, such as seizures, PHN, diabetic peripheral neuropathy, pain, restless-leg syndrome, essential tremor, bipolar disorder, migraine prophylaxis, and the symptoms associated with hormonal imbalances and chemotherapy."

Problems solved by technology

Furthermore, the slower release rate allows for a slower rise in peak plasma levels, which may be associated with side effects.

Method used

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  • Gastric retentive gabapentin dosage forms and methods for using same
  • Gastric retentive gabapentin dosage forms and methods for using same
  • Gastric retentive gabapentin dosage forms and methods for using same

Examples

Experimental program
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Effect test

example 1

[0192]Gastric retentive gabapentin tablets were manufactured using a dry blend process, and hand made on a Carver Auto C Press (Fred Carver, Inc., Indiana). The dry blend process consisted of blending all of the ingredients in a plastic bag, and compressing into a 1000 mg tablet (600 mg gabapentin dose) using a 0.7086″×0.3937″ Mod. Oval die (Natoli Engineering, St. Charles, Mo.). The parameters for the operation of the Carver Auto C Press were as follows: 4000 lbs force, 0-second dwell time (the setting on the Carver Press), and 100% pump speed. The formulation for the tablets is set froth in Table 1:

TABLE 1FORMULATION COMPOSITION (wt %)PEOMAGNE-SAMPLECOAGU-METHOCEL ®SIUMNO.GABAPENTINLANTK100MSTEARATE160.039.00.01260.024.314.71360.00.039.01

[0193]The dissolution was determined in USP apparatus 1 (40 mesh baskets), 100 rpm, in deionized water. Samples, 5 ml at each time-point, were taken without media replacement at 1, 4, and 8 hours. The resulting cumulative dissolution profile, base...

example 2

[0194]Gastric retentive gabapentin tablets were manufactured using a dry blend process, and hand made on a Carver Auto C Press (Fred Carver, Inc., Indiana). The dry blend process consisted of blending all of the ingredients in a plastic bag, and compressing into a 600 mg tablet (300 mg gabapentin) using a 0.6299″×0.3937″ Mod Oval die (Natoli Engineering, St. Charles, Mo.). The parameters for the operation of the Carver ‘Auto C’ Press were as follows: ˜2000-2500 lbs. force, 0-second dwell time (the setting on the Carver Press), and 100% pump speed. The formulation for the tablets is set forth in Table 3:

TABLE 3FORMULATION COMPOSITION (wt %)SAMPLEAC-PEOMETHOCEL ®MAGNESIUMNO.TIVECOAGULANTK15MSTEARATE450.024.524.501

[0195]The dissolution was determined in USP apparatus 1 (40 mesh baskets), 100 rpm, in deionized water. Samples, 5 ml at each time-point, were taken without media replacement at 1, 2, 4, 6, 8 and 10 hours. The resulting cumulative dissolution profile, based upon a theoretical...

example 3

[0196]Three gastric retentive gabapentin formulations were manufactured utilizing a standard granulation technique. The formulations manufactured are shown Table 5.

TABLE 5GR GABAPENTIN FORMULATIONSGABAPENTIN GR6,GABAPENTIN GR8,GABAPENTIN GR8,300-MG300-MG600-MG(GR6. 300-MG)(GR8, 300-MG)(GR8, 600-MG)44.76% Gabapentin44.76% Gabapentin61.11% Gabapentin16.46% METHOCEL ®21.99% METHOCEL ®7.59% METHOCEL ®K4M, premiumK15M, premiumK15M, premium21.99% SENTRY ®21.99% SENTRY ®27.09% SENTRY ®POLYOX ® WSR 303, NF FPPOLYOX ® WSR Coagulant,POLYOX ® WSR 303, NF FPNF FP12.98% AVICEL ®7.49% AVICEL ®0.00% AVICEL ®PH-101, NFPH-101, NFPH-101, NF2.75% METHOCEL ®2.75% METHOCEL ®3.22% METHOCEL ®E5, premiumE5, premiumE5, premium1.00% Magnesium Stearate,1.00% Magnesium Stearate,1.00% Magnesium Stearate,NFNFNF670-mg670-mg982-mg0.3937″× 0.6299″0.3937″× 0.6299″0.4062″× 0.75″Mod OvalMod OvalMod Cap

[0197]The dissolution profiles, as determined by USP Apparatus 1 (100 rpm) in modified simulated gastric fluid, for th...

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Abstract

Provided is a method of treating a patient suffering from a pain state by administering to the patient a gastric retentive dosage form of gabapentin that is capable of administration in once-daily or twice daily dosing regimens. By reducing the need to administer gabapentin from the thrice-daily administrations characteristic of immediate release gabapentin, the gastric retentive gabapentin dosage forms provided herein have the advantages of improving patient compliance for gabapentin treatment. In addition to the foregoing, the gastric retentive gabapentin dosages forms also exhibit decreased blood plasma concentrations and increased bioavailability throughout the dosing regimen.

Description

RELATED APPLICATIONS[0001]This application claims priority to pending U.S. Ser. No. 11 / 348,134, filed Dec. 29, 2006, which claims priority to U.S. Provisional Application Ser. No. 60 / 852,534 filed Oct. 17, 2006, the disclosures of which are incorporated herein by reference.FIELD OF THE INVENTION[0002]The invention relates to gastric retentive gabapentin dosage forms and methods of using them to reduce or eliminate gabapentin-induced side effects. For example, the dosage forms of the invention can be used to reduce or eliminate the side effects associated with treatment of non-nociceptive pain states.BACKGROUND OF THE INVENTION[0003]Gabapentin (1-(aminomethyl)cyclohexane acetic acid) is a 3-substituted γ-aminobutyric acid (“GABA”) analog that was approved in the United States on Dec. 30, 1993 as NEURONTIN® (Pfizer Inc., New York, N.Y.), an immediate release dosage form of gabapentin for use as adjunctive therapy in the treatment of partial seizures in children and adults, and was sub...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/195
CPCA61K9/2009A61K9/2013A61K9/2027A61K9/2031A61K9/284A61K31/195A61K9/2054
Inventor BERNER, BRETHOU, SUI YUEN EDDIEGANA, THEOPHILUS J.CRAMER, MARILOU S.
Owner DEPOMED SYST INC
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