OPTIMAL POLYMER MIXTURES FOR GASTRIC RETENTIVE TABLETS

US 20030104053A1
Filed: 10/25/2001
Published: 06/05/2003
Est. Priority Date: 10/25/2001
Status: Active Grant

First Claim

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1. A controlled-release oral drug dosage form for releasing a drug into at least a portion of a region defined by the stomach and the upper gastrointestinal tract, said dosage form comprising a solid monolithic matrix with said drug dispersed therein, said matrix comprising a combination of poly(ethylene oxide) and hydroxypropyl methylcellulose at a weight ratio that causes said matrix to swell upon contact with gastric fluid to a size large enough to provide gastric retention.

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Abstract

Unit dosage form tablets for the delivery of pharmaceuticals are formed of the pharmaceutical dispersed in a solid unitary matrix that is formed of a combination of poly(ethylene oxide) and hydroxypropyl methylcellulose. The combination offers unique benefits in terms of release rate control and reproducibility while allowing both swelling of the tablet to effect gastric retention and gradual disintegration of the tablet to clear the tablet from the gastrointestinal tract after release of the drug has occurred.

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20 Claims

1. A controlled-release oral drug dosage form for releasing a drug into at least a portion of a region defined by the stomach and the upper gastrointestinal tract, said dosage form comprising a solid monolithic matrix with said drug dispersed therein, said matrix comprising a combination of poly(ethylene oxide) and hydroxypropyl methylcellulose at a weight ratio that causes said matrix to swell upon contact with gastric fluid to a size large enough to provide gastric retention.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
- - 2. A controlled-release oral drug dosage form in accordance with claim 1 in which said matrix swells by at least about 20% of its original size within 30 minutes upon immersion in gastric fluid and to reach at least about 90% of its maximum size within 8 hours.
  - 3. A controlled-release oral drug dosage form in accordance with claim 1 in which said drug has a solubility in water that exceeds one part of said drug per ten parts of water, by weight, said poly(ethylene oxide) has a viscosity average molecular weight of from about 2,000,000 to about 10,000,000 daltons, and said hydroxypropyl methylcellulose has a viscosity of from about 4,000 centipoise to about 200,000 centipoise, measured as a 2% solution in water.
  - 4. A controlled-release oral drug dosage form in accordance with claim 1 in which said drug has a solubility in water that exceeds one part of said drug per ten parts of water, by weight, said poly(ethylene oxide) has a viscosity average molecular weight of from about 2,000,000 to about 10,000,000 daltons, and said hydroxypropyl methylcellulose has a viscosity of from about 50,000 centipoise to about 200,000 centipoise, measured as a 2% solution in water.
  - 5. A controlled-release oral drug dosage form in accordance with claim 1 in which said drug has a solubility in water that exceeds one part of said drug per ten parts of water, by weight, said poly(ethylene oxide) has a viscosity average molecular weight of from about 4,000,000 to about 7,000,000 daltons, and said hydroxypropyl methylcellulose has a viscosity of from about 80,000 centipoise to about 120,000 centipoise, measured as a 2% solution in water.
  - 6. A controlled-release oral drug dosage form in accordance with claim 3 in which said drug has a solubility in water that exceeds one part of said drug per three parts of water, by weight.
  - 7. A controlled-release oral drug dosage form in accordance with claim 1 in which said drug has a solubility in water that is less than one part of said drug per ten parts of water, by weight, said poly(ethylene oxide) has a viscosity average molecular weight of from about 100,000 to about 5,000,000 daltons, and said hydroxypropyl methylcellulose has a viscosity of from about 1,000 centipoise to about 100,000 centipoise, measured as a 2% solution in water.
  - 8. A controlled-release oral drug dosage form in accordance with claim 1 in which said drug has a solubility in water that is less than one part of said drug per ten parts of water, by weight, said poly(ethylene oxide) has a viscosity average molecular weight of from about 500,000 to about 2,500,000 daltons, and said hydroxypropyl methylcellulose has a viscosity of from about 4,000 centipoise to about 30,000 centipoise, measured as a 2% solution in water.
  - 9. A controlled-release oral drug dosage form in accordance with claim 8 in which said drug has a solubility in water ranging from about 0.05% to about 10% by weight.
  - 10. A controlled-release oral drug dosage form in accordance with claim 8 in which said drug has a solubility in water ranging from about 0.01% to about 5% by weight.
  - 11. A controlled-release oral drug dosage form in accordance with claim 1 in which the weight ratio of said poly(ethylene oxide) to hydroxypropyl methylcellulose is within the range of from about 1:
    - 3 to about 3;
      
      1.
  - 12. A controlled-release oral drug dosage form in accordance with claim 1 in which the weight ratio of said poly(ethylene oxide) to hydroxypropyl methylcellulose is within the range of from about 1:
    - 2 to about 2;
      
      1.
  - 13. A controlled-release oral drug dosage form in accordance with claim 1 in which the weight ratio of said poly(ethylene oxide) and hydroxypropyl methylcellulose in combination constitute from about 15% to about 90% by weight of said dosage form.
  - 14. A controlled-release oral drug dosage form in accordance with claim 1 in which said poly(ethylene oxide) and hydroxypropyl methylcellulose in combination constitute from about 30% to about 65% by weight of said dosage form.
  - 15. A controlled-release oral drug dosage form in accordance with claim 1 in which said poly(ethylene oxide) and hydroxypropyl methylcellulose in combination constitute from about 40% to about 50% by weight of said dosage form.
  - 16. A controlled-release oral drug dosage form in accordance with claim 1 in which said drug is a member selected from the group consisting of metformin hydrochloride, losartan potassium, ciprofloxacin, sodium valproate, valproic acid, and gabapentin.
  - 17. A controlled-release oral drug dosage form in accordance with claim 16 in which said drug is metformin hydrochloride.
  - 18. A controlled-release oral drug dosage form in accordance with claim 16 in which said drug is losartan potassium.
  - 19. A controlled-release oral drug dosage form in accordance with claim 16 in which said drug is ciprofloxacin.
  - 20. A controlled-release oral drug dosage form in accordance with claim 16 in which said drug is gabapentin.

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Current Assignee
Assertio Therapeutics, Inc. (Assertio Holdings, Inc.)
Original Assignee
Depomed Incorporated (Assertio Holdings, Inc.)
Inventors
Chau, Mei, Padua, Aimee, Berner, Bret, Gusler, Gloria

Granted Patent

US 6,723,340 B2
Time in Patent Office

Days
Field of Search
US Class Current

424/468
CPC Class Codes

A61K 9/0065   Forms with gastric retentio...

A61K 9/2031   obtained otherwise than by ...

A61K 9/2054   Cellulose; Cellulose deriva...

A61P 1/00   Drugs for disorders of the ...

A61P 1/04   for ulcers, gastritis or re...

A61P 1/06   Anti-spasmodics, e.g. drugs...

A61P 31/04   Antibacterial agents

A61P 35/00   Antineoplastic agents

OPTIMAL POLYMER MIXTURES FOR GASTRIC RETENTIVE TABLETS

First Claim

7 Assignments

0 Petitions

Accused Products

Abstract

182 Citations

20 Claims

Specification

Solutions

Use Cases

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OPTIMAL POLYMER MIXTURES FOR GASTRIC RETENTIVE TABLETS

First Claim

7 Assignments

Subscription Required

Subscription Required

0 Petitions

Subscription Required

Accused Products

Subscription Required

Abstract

182 Citations

20 Claims

Specification

Subscription Required

Solutions

Use Cases

Quick Links