Sustained release pharmaceutical compositions

Claim 2

A sustained release pharmaceutical composition comprising a compressed core, a seal coating surrounding the core and a sugar coating surrounding the seal coated core wherein, (a) the core comprises propranolol or a pharmaceutically acceptable acid addition salt thereof in an amount of about 20% to about 70% by weight of the core, at least one pharmaceutically acceptable water soluble polymer selected from the group consisting of hydroxypropyl methyl cellulose, hydroxypropyl cellulose, xanthan gum and karaya gum, and at least one pharmaceutically acceptable water insoluble polymer mixture selected from the group consisting of ethylcellulose and ethyl cellulose and at least one of carboxypolymethylene, hydroxypropyl methylcellulose phthalate and hydroxypropylcellulose, said polymers in an amount of about 30% to about 72% by weight of the core; (b) the seal coating comprises an enteric coating material; (c) and the sugar coating comprises sugar and a loading dose of said propranolol; and with the proviso that when the water soluble polymer is only hydroxypropyl methylcellulose then the water insoluble polymer is not only ethylcellulose, and that when the water insoluble polymer is only ethylcellulose then the water soluble polymer is not only hydroxypropyl methylcellulose.

Claim 3

The composition of claim 1 in which the seal coating comprises polyvinylacetate phthate.

Claim 4

The composition of claim 1 wherein the sugar coating further comprises at least one drug used in adjunct therapy with a β-adrenergic blocking agent.

Claim 5

The composition of claim 1 wherein the ratio of said propranolol in the core to said polymer is from about 0.3:1 to about 2.2:1 and the ratio of water soluble polymer to water insoluble polymer is from about 10:1 to about 1.5:1.

Claim 6

The composition of claim 3 or 4 wherein the ratio of said propranolol in the sugar coating to said propranolol in the core is from about 1:15 to about 1:4.3.

Claim 7

The composition of claim 3 or 4 comprising about 40-320 mg. of propranolol hydrochloride; wherein the ratio of propranolol in the sugar coating to propranolol in the core is from about 1:6 to about 1:8 and wherein the ratio of water soluble polymer to water insoluble polymer is from about 5:1 to about 1.5:1.

Claim 8

The composition of claim 6 wherein the sugar coating further comprises a therapeutically effective amount of at least one of hydrochlorothiazide and triameterene.

Claim 9

A sustained release pharmaceutical composition comprising a compressed core, a seal coating surrounding the core and a sugar coat surrounding the seal coated core wherein, (a) the core comprises propranolol or a pharmaceutically acceptable acid addition salt thereof in an amount of about 20% to about 70% by weight of the core, and the cellulose polymers hydroxypropyl methylcellulose and at least one of hydroxypropylcellulose and hydroxypropyl methylcellulose phthalate in an amount of about 30% to about 72% by weight of the core; (b) the seal coating comprises polyvinylacetate phthalate; and (c) the sugar coating comprises sugar and a loading dose of said propranolol.

Claim 10

A sustained release pharmaceutical composition comprising a compressed core, a seal coating surrounding the core and a sugar coat surrounding the seal coated core wherein, (a) the core comprises propranolol or a pharmaceutically acceptable acid addition salt thereof in an amount of about 20% to about 70% by weight of the core, and the cellulose polymers hydroxypropyl methylcellulose and at least one of hydroxypropylcellulose and hydroxypropyl methylcellulose phthalate in an amount of about 30% to about 72% by weight of the core; (b) the seal coating comprises polyvinylacetate phthalate; and (c) the sugar coating comprises sugar and a loading dose of said propranolol.

Claim 11

The composition of claim 8 comprising about 40-320 mg. of propranolol hydrochloride and wherein the ratio of propranolol in the sugar coating to propranolol in the core is from about 1:6 to about 1:8.

Claim 12

The composition of claim 9 in which the sugar coating further comprises at least one drug used in adjunct therapy with a β-adrenergic blocking agent.

Claim 13

A sustained release pharmaceutical composition comprising a compressed core, a seal coating surrounding the core and a sugar coating surrounding the seal coated core wherein, (a) the core comprises a therapeutically effective amount of at least one drug in amount of about 20% to about 70% by weight of the core, at least one pharmaceutically acceptable water soluble polymer selected from the group consisting of hydroxypropyl methyl cellulose, hydroxypropylcellulose, xanthan gum and karaya gum and at least one pharmaceutically acceptable water insoluble polymer mixture selected from the group consisting of ethyl cellulose and ethylcellulose and at least one of carboxypolymethylene, hydroxypropyl methylcellulose phthalate and hydroxypropylcellulose, said polymers in an amount of about 30% to about 72% by weight of the core; (b) the seal coating comprises an enteric coating material; (c) and the sugar coating comprises sugar and a loading dose of at least one drug contained in the core; and with the proviso that when the water soluble polymer is only hydroxypropyl methylcellulose then the water insoluble polymer is not only ethylcellulose, and that when the water insoluble polymer is only ethylcellulose then the water soluble polymer is not only hydroxypropyl methylcellulose; and wherein propranolol or a pharmaceutically acceptable salt thereof comprises at least one drug in both the core and the sugar coating.

Claim 14

A sustained release pharmaceutical composition comprising a compressed core, a seal coating surrounding the core and a sugar coating surrounding the seal coated core wherein, (a) the core comprises a therapeutically effective amount of at least one drug in amount of about 20% to about 70% by weight of the core, at least one pharmaceutically acceptable water soluble polymer selected from the group consisting of hydroxypropyl methyl cellulose, hydroxypropylcellulose, xanthan gum and karaya gum and at least one pharmaceutically acceptable water insoluble polymer mixture selected from the group consisting of ethyl cellulose and ethylcellulose and at least one of carboxypolymethylene, hydroxypropyl methylcellulose phthalate and hydroxypropylcellulose, said polymers in an amount of about 30% to about 72% by weight of the core; (b) the seal coating comprises an enteric coating material; (c) and the sugar coating comprises sugar and a loading dose of at least one drug contained in the core; and with the proviso that when the water soluble polymer is only hydroxypropyl methylcellulose then the water insoluble polymer is not only ethylcellulose, and that when the water insoluble polymer is only ethylcellulose then the water soluble polymer is not only hydroxypropyl methylcellulose; and wherein propranolol or a pharmaceutically acceptable salt thereof comprises at least one drug in both the core and the sugar coating.

Claim 15

The composition of claim 11 wherein the sugar coating further comprises at least one drug used in adjunct therapy with the drug contained in the core.

Claim 16

A sustained release pharmaceutical composition comprising a compressed core, a seal coating surrounding the core and a sugar coating surrounding the seal coated core wherein, (a) the core comprises a therapeutically effective amount of at least one drug in an amount of about 20% to about 70% by weight of the core, and the cellulose polymers hydroxypropyl methylcellulose and at least one of hydroxypropylcellulose and hydroxypropyl methylcellulose phthalate in an amount of about 30% to about 72% by weight of the core; (b) the seal coating comprises an enteric coating material; and (c) the sugar coating comprises sugar and a loading dose of at least one drug contained in the core; and wherein propranolol or a pharmaceutically acceptable salt thereof comprises at least one drug in both the core and the sugar coating.

Claim 17

A sustained release pharmaceutical composition comprising a compressed core, a seal coating surrounding the core and a sugar coating surrounding the seal coated core wherein, (a) the core comprises a therapeutically effective amount of at least one drug in an amount of about 20% to about 70% by weight of the core, and the cellulose polymers hydroxypropyl methylcellulose and at least one of hydroxypropylcellulose and hydroxypropyl methylcellulose phthalate in an amount of about 30% to about 72% by weight of the core; (b) the seal coating comprises an enteric coating material; and (c) the sugar coating comprises sugar and a loading dose of at least one drug contained in the core; and wherein propranolol or a pharmaceutically acceptable salt thereof comprises at least one drug in both the core and the sugar coating.

Claim 18

The composition of claim 13 wherein the sugar coating further comprises at least one drug used in adjunct therapy with the drug contained in the core.