Omeprazole compositions

Claim 2

An oral pharmaceutical preparation containing omeprazole, as the active ingredient, said preparation being enteric-coated pellets or enteric-coated tablet^ or capsules wherein the pellets may be dispensed in hard cfelatine capsules or formulated into tablets, said pellets or /cablets characterized in comprising: (A) an omepra/ole-containing, alkaline-reacting, core material; (B) at/least one inner or subcoating layer on said core material/said at least one inner or subcoating layer being inert/reacting and water soluble or rapidly disintegratable 2n water; and (C) an outer layer of an enteric coating on saia at least one inner or subcoating layer on the core material which renders s?.id preparation insoluble in acid media, the core material being such that an aqueous suspension or solution of the core material has a pH higher than that of a solution in which the enteric coating is just so/uble.

Claim 3

A preparation according to claim 1 wherein the alkaline-reacting core' material contains omeprazole together with an alkaline rea/ting compound, or an alkaline salt of omeprazole optionally together with an alkaline reacting . compound.

Claim 4

A preparation according to claim 1 wherein the alkaline-reacting core material contains omeprazole and pH- buffering alkaline compound rendering to the micro-environment of omepraz/le a pH of 7-12.

Claim 5

/A preparation according to claim 1 wherein the alkaline-reacting core material contains an alkaline salt of omep/azole such as the sodium, potassium, mactRjss$»s^ calcium or ./ammonium salt AS AMENDED 32 220C3G What we claim is: An oral pharmaceutical preparation containing omeprazole as the active ingredient, said preparation being enteric-coated pellets (wherein the enteric-coated pellets may be dispensed in hard gelatine capsules or formulated into tablets) or enteric-coated tablets said pellets or tablets characterised in comprising: (A) an omeprazole containing alkaline reacting core material; (B) at least one inner or subcoating layer on said core material, said at least one inner or sub coating layer being inert reacting and water soluble or rapidly disintegratable in water; and (C) an outer layer of an enteric coating on said at least one inner or sub coating layer on the core material which renders said preparation insoluble in acid media, the core material being such that an aqueous suspension or solution of the core material has a pH higher than that of a solution in which the enteric coating is just soluble. A preparation according to claim 1 wherein the alkaline-reacting core material contains omeprazole together with an alkaline reacting compound, or an alkaline salt of omeprazole optionally together with an alkaline reacting . compound. A preparation according to claim 1 wherein the alkaline-reacting core material contains omeprazole and a pH-buffering alkaline compound rendering to the micro-environment of omeprazole a pH of 7-12. A preparation according to claim 1 wherein the alkaline-reacting core material contains an alkaline salt of omeprazole such as the sodium, potassium, maao«s$asw calcium or ammonium salt. 220C;ib' SOW AMENDED 33 /

Claim 6

A preparation according to claim 1 wherein the / alkaline-reacting core material contains an alkaline salt of omeprazole mixed with an inert, alkaline compound. /

Claim 7

A preparation according to claim 5 wherein the alkaline compound comprises one or more of magnesium oxiue, hydroxide or carbonate; aluminium hydroxide; aluminium, calcium, sodium or potassium carbonate, phosphate or citrate; j£h& composite 5 substance aluminium/magnesium compounds / [Al203.6MgO.C02•12H20 or MgO.A1203.2SiO/;nH20], where n is not an integer and^less than 2.

Claim 8

A preparation according to/any one of claims 1 to 6 wherein the subcoating layer(s) comprises tablet excipients which are soluble or rapidly disintegratable in water and/or polymeric, water soluble, filin-forming compounds, optionally 5 containing pH-buffering, alkaline compounds.

Claim 9

A preparation according to any one of claims 1 to 6 wherein the subcoating /ayer(s) comprises one or more of magnesium oxide, magnesium hydroxide or the composite substance [A1203.6Mg02.12H20 at MgO.Al203.2Si02.nH20], 5 wherein n is not anr integer and [less than 2.

Claim 10

A preparation according to any one of claims 1 to 6 wherein the subcoating layer(s) comprises hydroxypropyl methylcellulose, hydroxypropyl cellulose or polyvinylpyrrolidone.

Claim 11

a preparation according to any one of claims 1 to 9 whereir/ the subcoating comprises two or more sub-coating layers. 22oc:;b' AS AMENDED 33 5 . A preparation according to claim 1 wherein the alkaline-reacting core material contains an alkaline salt of omeprazole mixed with an alkaline reacting, otherwise inert pharmaceutically acceptable compound. A preparation according to claim 5 wherein the alkaline compound comprises one or more of magnesium oxide, hydroxide or carbonate; aluminium hydroxide; aluminium, calcium, sodium or potassium carbonate, phosphate or citrate; the composite substance aluminium/magnesium compounds [Al203.6MgO.CO2.12H2O or MgO.Al203.2Si02.nH20], where n is not an integer and^less than 2. A preparation according to any one of claims 1 to 6 wherein the subcoating layer(s) comprises tablet excipients which are soluble or rapidly disintegratable in water and/or polymeric, water soluble, film-forming compounds, optionally containing pH-buffering, alkaline compounds. A preparation according to any one of claims 1 to 6 wherein the subcoating layer(s) comprises one or more of magnesium oxide, magnesium hydroxide or the composite substance [Al203.6Mg02.12H20 or MgO.Al203.2Si02.nH20], -IS wherein n is not an integer and less than 2. 9 . A preparation according to any one of claims 1 to 6 wherein the subcoating layer(s) comprises hydroxypropyl methylcellulose, hydroxypropyl cellulose or polyvinylpyrrolidone. A preparation according to any one of claims 1 to 9 wherein the subcoating comprises two or more sub-coating layers. SOW AMENDED 34 22009 6

Claim 12

A preparation according to any one of claimsr 1 to 10 wherein the enteric coating comprises hydroxy propyl methylcellulose phthalate, cellulose acetate phthalate/ copolymerized methacrylic acid/methacrylic acid methyl ester/or polyvinyl acetate phthalate, optionally containing a plasticizer.

Claim 13

A preparation according to any one/of claims 1 to 11 wherein the water content of the final dc/sage form containing omeprazole does not exceed 1.5% by weignt.

Claim 14

A process for the preparation of an oral pharmaceutical formulation containing omeprazole,/wherein cores of omeprazole-containing, alkaline-reacting material as defined in any one of claims 1 to 12 are coated with ame or more inert-reacting, inner or subcoating layers as jaefined in any one of claims 1 to 12, whereafter the subcoatedycores are further coated with an enteric coating as defined in any one of claims 1 to 12.

Claim 15

An oral pharmaceutical preparation obtained by the process according to cl/im 13.

Claim 16

An oral pharmaceutical preparation obtained by the process according to cl/im 13.

Claim 17

The use of a/preparation according to any one of claims 1 to 12 and 14 for tme manufacture of a medicament for the treatment of gastrointestinal diseases.

Claim 18

A method far the treatment of gastrointestinal disease in an animal other/than a human, characterized in that a preparation according to any one of claims 1 to 12 and 14 is administered/to the animal in need of such treatment in a therapeutically effective amount. AKTIEBOLAGET HASSLE By its Patent Attorneys HENRY HUGHES LIMITED Byv(M€{ku^o ^ X //I ' ' 28M Akr/'jQ::;:'; \ /< V / , v 220096 AS AMENDED 34 A preparation according to any one of claims 1 to 10 wherein the enteric coating comprises hydroxy propyl methylcellulose phthalate, cellulose acetate phthalate, copolymeirized methacrylic acid/methacrylic acid methyl ester or polyvinyl acetate phthalate, optionally containing a plasticizer. A preparation according to any one of claims 1 to 11 wherein the water content of the final dosage form containing omeprazole does not exceed 1.5% by weight. A process for the preparation of an oral pharmaceutical formulation containing omeprazole, wherein cores of omeprazole-containing, alkaline-reacting material as defined in any one of claims 1 to 12 are coated with one or more inert-reacting, inner or subcoating layers as defined in any one of claims 1 to 12, whereafter the subcoated :or'es are further coated with an enteric coating as defined in any one of claims 1 to 12. An oral pharmaceutical preparation obtained by the process according to claim 13. The use of a preparation according to any one of claims 1 to 12 and 14 for the manufacture of a medicament for the treatment of gastrointestinal diseases. 16* A method for the treatment of gastrointestinal disease in an animal other than a human, characterized in that a preparation according to any one of claims 1 to 12 and 14 is administered to the animal in need of such treatment in a therapeutioal1y effective amount. AKTIEBOLAGET HASSLE By its Patent Attorneys HENRY HUGHES LIMITED By:A L.