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Claims for Patent: 6,548,084

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Claims for Patent: 6,548,084

Title: Controlled release compositions
Abstract:A controlled release or delayed release formulation contains a selective serotonin reuptake inhibitor (SSRI) such as paroxetine.
Inventor(s): Leonard; Graham Stanley (St Albans, GB), Elder; David Philip (Hertford, GB)
Assignee: SmithKline Beecham plc (GB)
Application Number:09/391,796
Patent Claims: 1. A method of reducing the incidence of nausea and vomiting associated with the administration of a selective serotonin reuptake inhibiting compound selected from fluvoxamine and sertraline, or a pharmaceutically acceptable salt thereof, which method consists of administering an effective amount of a selective serotonin reuptake inhibiting compound in a controlled release, delayed release or a combination of a controlled release and delayed release swallow pharmaceutical formulation that, upon oral administration, releases the selective serotonin reuptake inhibiting compound predominantly in the small intestine.

2. The method of claim 1 in which the formulation is an enteric coated controlled release bilayer tablet.

3. A method of reducing the incidence of nausea and vomiting associated with the administration of a selective serotonin reuptake inhibiting compound selected from paroxetine, fluoxetine, fluvoxamine and sertraline, or a pharmaceutically acceptable salt thereof, which method consists of administering an effective amount of the selective serotonin reuptake inhibiting compound as a polymeric controlled release composition comprising a reaction complex formed by the interaction of (1) a calcium polycarbophil component which is a water-swellable, but water insoluble, fibrous cross-linked carboxy-functional polymer, said polymer containing (a) a plurality of repeating units of which at least about 80% contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5% cross-linking agent substantially free from polyalkenyl polyether, said percentages being based upon the weights of unpolymerized repeating unit and cross-linking agent, respectively with (2) water, in the presence of a selective serotonin reuptake inhibiting compound.

4. A method of reducing the incidence of nausea and vomiting associated with the administration of a selective serotonin reuptake inhibiting compound paroxetine, or a pharmaceutically acceptable salt thereof, which method consists of administering an effective amount of the selective serotonin reuptake inhibiting compound as a polymeric controlled release composition comprising a reaction complex formed by the interaction of (1) a calcium polycarbophil component which is a water-swellable, but water insoluble, fibrous cross-linked carboxy-functional polymer, said polymer containing (a) a plurality of repeating units of which at least about 80% contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5% cross-linking agent substantially free from polyalkenyl polyether, said percentages being based upon the weights of unpolymerized repeating unit and cross-linking agent, respectively with (2) water, in the presence of a selective serotonin reuptake inhibiting compound.

5. A method of reducing the incidence of nausea and vomiting associated with the administration of a selective serotonin reuptake inhibiting compound which method consists of administering an effective amount of a selective serotonin reuptake inhibiting compound in a controlled release, delayed release or a combination of a controlled release and delayed release swallow pharmaceutical formulation that, upon oral administration, releases the selective serotonin reuptake inhibiting compound predominantly in the small intestine, said formulation comprising (a) a deposit-core comprising an effective amount of a selective serotonin reuptake inhibiting compound and having defined geometric form, and (b) a support-platform applied to said deposit-core, wherein said deposit-core contains at least the active substance, and at least one member selected from the group consisting of (1) a polymeric material which swells on contact with water or aqueous liquids and a gellable polymeric material wherein the ratio of the said swellable polymeric material to said gellable polymeric materials in the range 1:9 to 9:1, and (2) a single polymeric material having both swelling and gelling properties, and wherein the support-platform is an elastic support, applied to said deposit-core so that it partially covers the surface of the deposit-core and follows changes due to hydration of the deposit-core and is slowly soluble and/or slowly gellable in aqueous fluids.

6. A method of reducing the incidence of nausea and vomiting associated with the administration of a selective serotonin reuptake inhibiting compound paroxetine or a pharmaceutically acceptable salt thereof, which method consists of administering an effective amount of a selective serotonin reuptake inhibiting compound in a controlled release, delayed release or a combination of a controlled release and delayed release swallow pharmaceutical formulation that, upon oral administration, releases the selective serotonin reuptake inhibiting compound predominantly in the small intestine, said formulation comprising (a) a deposit-core comprising an effective amount of the selective serotonin reuptake inhibiting compound and having defined geometric form, and (b) a support-platform applied to said deposit-core, wherein said deposit-core contains at least the active substance, and at least one member selected from the group consisting of (1) a polymeric material which swells on contact with water or aqueous liquids and a gellable polymeric material wherein the ratio of the said swellable polymeric material to said gellable polymeric materials in the range 1:9 to 9:1, and (2) a single polymeric material having both swelling and gelling properties, and wherein the support-platform is an elastic support, applied to said deposit-core so that it partially covers the surface of the deposit-core and follows changes due to hydration of the deposit-core and is slowly soluble and/or slowly gellable in aqueous fluids.

7. A controlled release, delayed release or a combination of a controlled release and delayed release swallow pharmaceutical formulation that reduces the incidence of nausea and vomiting associated with the administration of a selective serotonin reuptake inhibiting compound that, upon oral administration, releases the selective serotonin reuptake inhibiting compound predominantly in the small intestine, which formulation is a polymeric composition comprising a reaction complex formed by the interaction of (1) a calcium polycarbophil component which is a water-swellable, but water insoluble, fibrous cross-linked carboxy-functional polymer, said polymer containing (a) a plurality of repeating units of which at least about 80% contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5% cross-linking agent substantially free from polyalkenyl polyether, said percentages being based upon the weights of unpolymerized repeating unit and cross-linking agent, respectively with (2) water, in the presence of a selective serotonin reuptake inhibiting compound.

8. A controlled release, delayed release or a combination of a controlled release and delayed release swallow pharmaceutical formulation that reduces the incidence of nausea and vomiting associated with the administration of the selective serotonin reuptake inhibiting compound paroxetine, or a pharmaceutically acceptable salt thereof that, upon oral administration, releases the selective serotonin reuptake inhibiting compound predominantly in the small intestine, which formulation is a polymeric composition comprising a reaction complex formed by the interaction of (1) a calcium polycarbophil component which is a water-swellable, but water insoluble, fibrous cross-linked carboxy-functional polymer, said polymer containing (a) a plurality of repeating units of which at least about 80% contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5% cross-linking agent substantially free from polyalkenyl polyether, said percentages being based upon the weights of unpolymerized repeating unit and cross-linking agent, respectively with (2) water, in the presence of the selective serotonin reuptake inhibiting compound.

9. A controlled release, delayed release or a combination of a controlled release and delayed release swallow pharmaceutical formulation that reduces the incidence of nausea and vomiting associated with the administration of the selective serotonin reuptake inhibiting compound that, upon oral administration, releases the selective serotonin reuptake inhibiting compound predominantly in the small intestine, which formulation comprises (a) a deposit-core comprising an effective amount of the active substance and having defined geometric form, and (b) a support-platform applied to said deposit-core, wherein said deposit-core contains at least the active substance, and at least one member selected from the group consisting of (1) a polymeric material which swells on contact with water or aqueous liquids and a gellable polymeric material wherein the ratio of the said swellable polymeric material to said gellable polymeric materials in the range 1:9 to 9:1, and (2) a single polymeric material having both swelling and gelling properties, and wherein the support-platform is an elastic support, applied to said deposit-core so that it partially covers the surface of the deposit-core and follows changes due to hydration of the deposit-core and is slowly soluble and/or slowly gellable in aqueous fluids.

10. A controlled release, delayed release or a combination of a controlled release and delayed release swallow pharmaceutical formulation that reduces the incidence of nausea and vomiting associated with the administration of the selective serotonin reuptake inhibiting compound paroxetine, or a pharmaceutically acceptable salt thereof that, upon oral administration, releases the selective serotonin reuptake inhibiting compound predominantly in the small intestine, which formulation comprises (a) a deposit-core comprising an effective amount of the active substance and having defined geometric form, and (b) a support-platform applied to said deposit-core, wherein said deposit-core contains at least the active substance, and at least one member selected from the group consisting of (1) a polymeric material which swells on contact with water or aqueous liquids and a gellable polymeric material wherein the ratio of the said swellable polymeric material to said gellable polymeric materials in the range 1:9 to 9:1, and (2) a single polymeric material having both swelling and gelling properties, and wherein the support-platform is an elastic support, applied to said deposit-core so that it partially covers the surface of the deposit-core and follows changes due to hydration of the deposit-core and is slowly soluble and/or slowly gellable in aqueous fluids.

11. A process for preparing a controlled or delayed release formulation of a selective serotonin reuptake inhibiting compound, which comprises combining (1) a calcium polycarbophil component which is a water-swellable, but water insoluble, fibrous cross-linked carboxy-functional polymer, said polymer containing (a) a plurality of repeating units of which at least about 80% contain at least one carboxyl functionality, and (b) about 0.05 to about 1.5% cross-linking agent substantially free from polyalkenyl polyether, said percentages being based upon the weights of unpolymerised repeating unit and cross-linking agent, respectively, with (2) water, in the presence of a selective serotonin reuptake inhibiting compound.
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