Method for preparing preparations having controlled release of an active component

Claim 2

A process for producing a preparation comprising a plurality of granules each having a core and a unitary layer thereon containing at least one pharmaceutically active material which, on disintegration, release said pharmaceutically active material at a controlled rate, comprising applying to said cores in a continuous coating operation a solution or suspension containing at least one active compound and at least one pharmaceutically inactive release controlling substance over a period of time sufficient to cause said unitary layer of said active ingredient and inactive release controlling substance to form on each core to give granules of size 0.3-2 mm, during said time period the concentration of active ingredient being decreased in the solution or suspension from which the layer is formed by adding additional release controlling substance to the solution or suspension, whereby there results granules each having a layer containing an active ingredient in which layer the concentration of active ingredient decreased radially outwardly from the core to the outer surface of said layer.

Claim 3

A process according to claim 1, wherein said continuous coating is carried out by spraying said composition comprising active ingredient and inactive release controlling substance onto said core.

Claim 4

A process according to claim 1, wherein the concentration of active ingredient in said solution or suspension decreases continuously with time, whereby the concentration of active ingredient in the layer on said core decreases continuously toward the surface thereof.

Claim 5

A process according to claim 1, wherein the concentration of active ingredient in said solution or suspension is decreased during the time of coating in a discontinuous change, whereby a discontinuous gradient of concentration toward the surface of said layer is obtained.

Claim 6

A process according to claim 1, wherein the inactive release controlling substance has lipophilic characteristics.

Claim 7

A process according to claim 1, wherein said inactive release controlling substance is a water-soluble polymer.

Claim 8

A process according to claim 1, wherein the inactive release controlling substance is insoluble and dispersable in water.

Claim 9

A process according to claim 1, wherein said biologically active material is a therapeutically active component.

Claim 10

A process according to claim 1, wherein the core, before application of the outer layer, has a diameter of at least 0.05 mm.

Claim 11

A process for producing a preparation comprising a plurality of granules, each granule having a core and a unitary layer thereon containing at least one pharmaceutically active material which, on disintegration, release said pharmaceutically active material at a controlled rate, comprising applying to said cores in a continuous coating operation a solution or suspension containing at least one pharmaceutically active compound and at least one pharmaceutically inactive release controlling substance selected from the group consisting of waxes, fatty acids, fatty acid esters, fatty alcohols, polyethylene glycols, polyvinylpyrrolidones, polyvinylacetates, polyacrylates, polymethacrylates, cellulose derivatives, talcum and silicic acid, over a period of time sufficient to cause said unitary layer of said active ingredient and inactive release controlling substance to form on each core to give granules of size 0.3-2 mm, during said time period the concentration of active ingredient being decreased in the solution or suspension from which the layer is formed by adding additional release controlling substance to the solution or suspension, whereby there results granules each having a layer containing an active ingredient in which layer the concentration of active ingredient decreases radially outwardly from the core to the outer surface of said layer.

Claim 12

A process for producing a preparation comprising a plurality of granules, each granule having a core and a unitary layer thereon containing at least one pharmaceutically active material which, on disintegration, release said pharmaceutically active material at a controlled rate, comprising applying to said cores in a continuous coating operation a solution or suspension containing at least one pharmaceutically active compound and at least one pharmaceutically inactive release controlling substance selected from the group consisting of waxes, fatty acids, fatty acid esters, fatty alcohols, polyethylene glycols, polyvinylpyrrolidones, polyvinylacetates, polyacrylates, polymethacrylates, cellulose derivatives, talcum and silicic acid, over a period of time sufficient to cause said unitary layer of said active ingredient and inactive release controlling substance to form on each core to give granules of size 0.3-2 mm, during said time period the concentration of active ingredient being decreased in the solution or suspension from which the layer is formed by adding additional release controlling substance to the solution or suspension, whereby there results granules each having a layer containing an active ingredient in which layer the concentration of active ingredient decreases radially outwardly from the core to the outer surface of said layer.

Claim 13

A process for producing a preparation comprising a plurality of granules each having a core and a unitary layer thereon containing at least one biologically active material which, on disintegration, release said biologically active material at a controlled rate, comprising applying to said cores in a continuous coating operation a solution or suspension containing at least one active compound and at least one biologically inactive release controlling substance over a period of time sufficient to cause said unitary layer of said active ingredient and inactive release controlling substance to form on each core to give granules of size 0.3-2 mm, during said time period the concentration of active ingredient being decreased in the solution or suspension from which the layer is formed by adding additional release controlling substance to the solution or suspension, whereby there results granules each having a layer containing an active ingredient in which layer the concentration of active ingredient decreases radially outwardly from the core to the outer surface of said layer.

Claim 14

A process for producing a preparation comprising a plurality of granules each having a core and a unitary layer thereon containing at least one biologically active material which, on disintegration, release said biologically active material at a controlled rate, comprising applying to said cores in a continuous coating operation a solution or suspension containing at least one active compound and at least one biologically inactive release controlling substance over a period of time sufficient to cause said unitary layer of said active ingredient and inactive release controlling substance to form on each core to give granules of size 0.3-2 mm, during said time period the concentration of active ingredient being decreased in the solution or suspension from which the layer is formed by adding additional release controlling substance to the solution or suspension, whereby there results granules each having a layer containing an active ingredient in which layer the concentration of active ingredient decreases radially outwardly from the core to the outer surface of said layer.

Claim 15

A process for producing a preparation comprising a plurality of granules, each granule having a core and a unitary layer thereon containing at least one biologically active material which, on disintegration, release said biologically active material at a controlled rate, comprising applying to said cores in a continuous coating operation a solution or suspension containing at least one active compound and at least one biologically inactive release-controlling substance selected from the group consisting of waxes, fatty acids, fatty acid esters, fatty alcohols, polyethylene glycols, polyvinylpyrrolidones, polyvinylacetates, polyacrylates, polymethacrylates, cellulose derivatives, talcum and silicic acid, over a period of time sufficient to cause said unitary layer of said active ingredient and inactive release controlling substance to form on each core to give granules of size 0.3-2 mm, during said time period the concentration of active ingredient being decreased in the solution or suspension from which the layer is formed by adding additional release controlling substance or suspension, whereby there results granules each having the concentration of active ingredient decreases radially outwardly from the core to the outer surface of said layer.

Claim 16

A process for producing a preparation comprising a plurality of granules, each granule having a core and a unitary layer thereon containing at least one biologically active material which, on disintegration, release said biologically active material at a controlled rate, comprising applying to said cores in a continuous coating operation a solution or suspension containing at least one active compound and at least one biologically inactive release-controlling substance selected from the group consisting of waxes, fatty acids, fatty acid esters, fatty alcohols, polyethylene glycols, polyvinylpyrrolidones, polyvinylacetates, polyacrylates, polymethacrylates, cellulose derivatives, talcum and silicic acid, over a period of time sufficient to cause said unitary layer of said active ingredient and inactive release controlling substance to form on each core to give granules of size 0.3-2 mm, during said time period the concentration of active ingredient being decreased in the solution or suspension from which the layer is formed by adding additional release controlling substance or suspension, whereby there results granules each having the concentration of active ingredient decreases radially outwardly from the core to the outer surface of said layer.