# US 7,612,112 B2 · Methods of treatment using a gastric retained gabapentin dosage

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- Number: US 7,612,112 B2
- Document ID: US7612112B2
- Status: Granted
- Kind: B2
- Application number: 10/903,879
- Filed: 2004-07-30
- Published: 2005-03-24
- Granted: 2009-11-03
- Earliest claimed: 2001-10-25
- Assignees: Depomed, Inc.
- Inventors: Bret Berner; Sui Yuen Eddie Hou; Gloria M. Gusler
- Web page: https://patentgrep.com/patent/US7612112B2

## CPC

- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/0004: {Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas}
- A61K 9/0065: {Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus}
- A61K 31/195: having an amino group
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61M 31/002: {Devices for releasing a drug at a continuous and controlled rate for a prolonged period of time (artificial gland structures or devices A61F2/022; intra-uterine contraceptive devices A61F6/14; tampons for introducing into the vagina A61F13/20, A61L15/00; suppositories or bougies for intra-vaginal or intra-uterine application A61K9/02; physical forms of medicinal preparations for sustained or differential drug release A61K9/20, A61K9/50)}
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/06: Antimigraine agents
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61K 9/2031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/284: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone}
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)}
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 1

An extended release oral drug dosage form for releasing gabapentin, comprising:
a core comprising at least 800 mg of gabapentin, and
a semipermeable membrane surrounding the core, the semipermeable membrane comprising a plasticizer and being permeable to a fluid in an environment of use and substantially impermeable to unsolubilized gabapentin,
wherein the dosage form as formulated is of sufficient size for retention in the stomach in a fed mode for a period of at least about 5 hours, and wherein at least about 80 wt % of the gabapentin is released from the dosage form in about 5-12 hours via controlled release through the semipermeable membrane.

### Claim 2 (depends on 1)

The dosage form of claim 1, wherein the core comprises between about 800-1600 mg gabapentin.

### Claim 3 (depends on 1)

The dosage form of claim 1, wherein the semipermeable membrane comprises a material selected from the group consisting of acetaldehyde dimethyl acetate, acetaldehyde dimethylcellulose acetate, agar acetate, alkylene oxide and alkyl glycidyl ether copolymers, amylose triacetate, beta glucan acetate, beta glucan triacetate, cellulose esters, cellulose ethers, cellulose ester-ether polymers, mono-, di- and tricellulose acrylates, mono-, di- and tricellulose alkenylates, hydroxylated ethylene-vinyl acetate, polyamides, polyalkylene oxides, polyether and polyamide copolymers, polyglycolic acid, polylactic acid, poly(methacrylate) copolymer salts, cross-linked poly(sodium styrene sulfonate), crosslinked polystyrenes, polyurethanes, polyvinyl alcohol, crosslinked poly(vinylbenzyltrimethyl ammonium chloride), polyvinyl chloride, poly(vinylmethyl ether) copolymers, polyvinylpyrrolidone, propylcarbamate, sulfonated polystyrenes, and triacetate of locust gum bean.

### Claim 4 (depends on 3)

The dosage form of claim 3, wherein the semipermeable membrane comprises a material selected from the group consisting of cellulose esters, cellulose ethers, polyalkylene oxides, polyvinyl alcohol, and polyvinylpyrrolidone.

### Claim 5 (depends on 4)

The dosage form of claim 4, wherein the cellulose ester is selected from the group consisting of mono-, di- and tricellulose acetates, cellulose acetate butyl sulfonate, cellulose acetate butyrate, cellulose acetate chloroacetate, cellulose acetate dimethylaminoacetate, cellulose acetate ethyl carbamate, cellulose acetate ethyl carbonate, cellulose acetate ethyl oxalate, cellulose acetate laurate, cellulose acetate methyl carbamate, cellulose acetate methyl sulfonate, cellulose acetate octate, cellulose acetate phthalate, cellulose acetate propionate, cellulose acetate succinate, cellulose acetate p-toluene sulfonate, cellulose acetate valerate, cellulose propionate, cellulose propionate succinate, dimethyl cellulose acetate, mono-, di- and tricellulose acrylates, mono-, di- and tricellulose alkanylates, mono, di and tricellulose aroylates, cellulose triacylates, and cellulose diacylates.

### Claim 6 (depends on 4)

The dosage form of claim 4, wherein the cellulose ether is selected from the group consisting of ethyl cellulose, hydroxyethylcellulose, hydroxypropylcellulose, and methylcellulose.

### Claim 7 (depends on 1)

The dosage form of claim 1, wherein the plasticizer is selected from the group consisting of acetylated monoglycerides, dibutyl phthalate, diethyl phthalate, isopropyl phthalate, dimethyl phthalate, dactyl phthalate, dibutyl sebacate, dimethyl sebacate, esters, fatty acids, glycols, oils, glycerin, glycerol, glycerol monostearate, and triacetin.

### Claim 8 (depends on 7)

The dosage from of claim 7, wherein the plasticizer is selected from esters and fatty acids.

### Claim 9 (depends on 8)

The dosage from of claim 8, wherein the ester is selected from the group consisting of acetyl triethyl citrate, acetyl tributyl citrate, citrate ester, dibutyl sebacate, tetraethyl acetate, and triethyl citrate.

### Claim 10 (depends on 8)

The dosage from of claim 8, wherein the fatty acid is stearic acid.

### Claim 11 (depends on 1)

The dosage form of claim 1, wherein the semipermeable membrane comprises ethyl cellulose, stearic acid, and polyvinylpyrrolidone.

### Claim 12 (depends on 1)

The dosage form of claim 1, wherein the semipermeable membrane comprises ethyl cellulose, stearic acid, and hydroxypropylcellulose.

### Claim 13 (depends on 3)

The dosage form of claim 3, wherein the semipermeable membrane comprises polyvinyl alcohol.

### Claim 14 (depends on 13)

The dosage form of claim 13, wherein the polyvinyl alcohol is a blend of a water soluble polyvinyl alcohol and a water insoluble polyvinyl alcohol.

### Claim 15 (depends on 13)

The dosage form of claim 13, wherein the polyvinyl alcohol is crosslinked.

### Claim 16 (depends on 1)

The dosage form of claim 1, wherein the dosage form allows for the extended release of gabapentin in the stomach and small intestine of a mammal.

### Claim 17 (depends on 1)

The dosage form of claim 1, wherein at least 40 wt % of the gabapentin is retained in the dosage form after 1 hour.

### Claim 18

An extended release oral drug dosage form for releasing gabapentin into the stomach, duodenum and small intestine of a mammal, comprising:
a core comprising at least 800 mg of gabapentin, and
a semipermeable membrane surrounding the core, the semipermeable membrane comprising a plasticizer and being permeable to a fluid in an environment of use and substantially impermeable to unsolubilized gabapentin,
wherein the dosage form as formulated is of sufficient size for retention in the stomach in a fed mode for a period of at least about 5 hours, and wherein at least about 80 wt % of the gabapentin is released from the dosage form in about 5-12 hours via controlled release through the semipermeable membrane.