Oral therapeutic system having systemic action

• US RE34,990 E
• Filed: 10/08/1993
• Issued: 07/04/1995
• Est. Priority Date: 08/07/1986
• Status: Expired due to Term

• Current Assignee: Novartis Corporation (Novartis Ag)
• Original Assignee: Ciba-Geigy Corporation (Novartis Ag)
• Inventors: Ruttimann, Theresa, Khanna, Satish C.
• Primary Examiner(s): Webman, Edward J.
• Application Number:
  US08/133,814
• Time in Patent Office: 634 Days
• Field of Search: 424/484, 424/473, 424/485, 424/486, 424/488, 424/469
• US Class Current: 424/473
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

Abstract

The invention relates to a therapeutic system for peroral administration and having systemic action, which system is in the form of a coated and/or laminated mono-compartment system for administering carbamazepine. The therapeutic system comprises

(a) a wall made of a material which is permeable to water and impermeable to the components of the drug-containing core,

(b) a core containing finely particulate carbamazepine as drug and, as auxiliaries, a protective colloid that inhibits the crystal growth of carbamazepine in the presence of water, a swellable hydrophilic polymer and, optionally, a water-soluble compound for inducing osmosis and/or further pharmaceutically acceptable excipients, and

(c) a passageway through the wall (a) for delivering the core components to the environmental body fluid. The therapeutic system can be used as an anticonvulsive for the treatment of convulsive states, especially epileptic states.

Claims

1. An oral therapeutic system for administering carbamazepine comprising

(a) a wall made of acylated cellulose which is permeable to water but impermeable to the components of the drug containing core and to the ions present in gastric or intestinal juices;

(b) a core containing finely particulate carbamazepine as a drug, hydroxypropylmethyl cellulose as protective colloid, a swellable hydrophilic polymer selected from the group consisting of poly-N-vinyl-2-pyrrolidone, polyvinyl alcohol, alkylene oxide homopolymers, methyl cellulose, ethyl cellulose, hydroxypropyl cellulose, the copolymer of vinylpyrrolidone and vinyl acetate, the mixture of the copolymer of vinylpyrrolidone and vinyl acetate and the homopolymer of ethylene oxide and, a water soluble compound for inducing osmosis; and

(c) a passageway through the wall (a) for delivering the components present in the core to the environmental gastric or intestinal juices.

2. An oral therapeutic system according to claim 1, comprising

(a) a wall made of acylated cellulose which is permeable to water but impermeable to the components of the drug-containing core and to the ions present gastric or intestinal juices,

(b) a core containing finely particulate carbamazepine as drug, hydroxymethyl cellulose as protective colloid, a 1:

1 mixture % by weight of a copolymer of vinylpyrrolidone and vinyl acetate and a homopolymer of ethylene oxide as swellable hydrophilic polymer, and and

(c) passageway through the wall (a) for delivering the components present in the core to the environmental aqueous body fluid.

3. An oral therapeutic system according to claim 1, comprising

(a) a wall made of cellulose acetate which is permeable to water but impermeable to the components of the drug-containing core and to the ions present in gastric or intestinal juices,

(b) a core containing carbamazepine as drug, hydroxypropyl methylcellulose as protective colloid, a 1:

1 mixture % by weight of a copolymer of vinylpyrrolidone and vinyl acetate having a molecular weight of 60.000±

15,000 and having a monomer ratio of 60;

40% by weight and a homopolymer of ethylene oxide having a degree of polymerisation of 2000 to 100,000 as swellable hydrophilic polymer, and

(c) a passageway through the wall (a) for delivering the components present in the core to the environmental gastric or intestinal juices.

4. An oral therapeutic system according to claim 1, which contains anhydrous microcrystals of carbamazepine.

5. An oral therapeutic system according to claim 1, which contains anhydrous microcrystals of carbamazepine having a size of up to 20 μ

m, and hydroxypropyl methylcellulose as protective colloid.

6. The therapeutic system of claim 2 further comprising a compound for inducing osmosis selected from sodium chloride, potassium chloride, glucose, and mannitol.

7. The therapeutic system of claim 3 further comprising a compound for inducing osmosis selected from sodium chloride, potassium chloride, glucose and mannitol. .Iadd.

8. An oral therapeutic system for administrating carbamazepine comprising

(a) a wall made of acylated cellulose which is permeable to water but impermeable to the components of the drug containing core and to the ions present in gastric or intestinal juices;

(b) a core containing finely particulate carbamazepine as a drug, hydroxypropylmethyl cellulose as protective colloid, a swellable hydrophilic polymer selected from the group consisting of poly-N-vinyl-2-pyrrolidone, polyvinyl alcohol, alkylene oxide homopolymers, methyl cellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, the copolymer of vinyl pyrrolidone and vinyl acetate, the mixture of the copolymer of vinylpyrrolidone and vinyl acetate and the homopolymer of ethylene oxide and, a water soluble compound for inducing osmosis; and

(c) a passageway through the wall (a) for delivering the components present in the core to the environmental gastric or intestinal juices. .Iaddend. .Iadd.9. The oral therapeutic system of claim 8 wherein 2 swellable hydrophilic polymers are present. .Iaddend. .Iadd.10. The oral therapeutic system of claim 8 wherein said carbamazepine is present as anhydrous microcrystals. .Iaddend. .Iadd.11. The oral therapeutic system of claim 10 wherein carbamazepine microcrystals have a size of up to 20um, and said protective colloid is hydroxypropyl methylcellulose. .Iaddend. .Iadd.12. The oral therapeutic system of claim 8 further comprising a compound for inducing osmosis selected from sodium chloride, potassium chloride, and carbohydrates. .Iaddend. .Iadd.13. The oral therapeutic system of claim 11 further comprising a compound for inducing osmosis selected from sodium chloride, potassium chloride, and carbohydrates. .Iaddend. .Iadd.14. The oral therapeutic system of claim 8 wherein said core comprises anhydrous carbamazepine, hydroxypropyl methylcellulose, hydroxyethylcellulose, and mannitol. .Iaddend. .Iadd.15. The oral therapeutic system of claim 8 wherein said wall comprises cellulose acetate, hydroxypropyl methylcellulose, and polyethylene glycol 8000. .Iaddend.