EP0148811A1 — Pharmaceutical composition

Claim 1

Independent Claim 93 words

Oral pharmaceutical composition having an improved release of the therapeutically active compound present independent from its solubility, characterized by a core comprising a therapeutically active compound in the form of a weak base or a weak acid, on which core there is applied a first inner layer of a diffusion membrane in the form of ethyl cellulose and/or a copolymer of polyethyl methacrylate- methyl methacrylate-trimethylammonium ethyl methacrylate chloride, and thereabove there is applied a second layer of at least one anionic polymer and/or fatty acid having a pk a of 4.5 to 7.

Claim 2

Dependent Claim 93 words

Oral pharmaceutical composition having an improved release of the therapeutically active compound present independent from its solubility, characterized by a core comprising a therapeutically active compound in the form of a weak base or a weak acid, on which core there is applied a first inner layer of a diffusion membrane in the form of ethyl cellulose and/or a copolymer of polyethyl methacrylate- methyl methacrylate-trimethylammonium ethyl methacrylate chloride, and thereabove there is applied a second layer of at least one anionic polymer and/or fatty acid having a pk a of 4.5 to 7.

Claim 3

Dependent Claim 23 words

Pharmaceutical composition according to claim 1, characterized in that the pk a of the material in the second layer is 5.5 to 6.5.

Claim 4

Dependent Claim 34 words

Pharmaceutical composition according to claim 1, characterized in that the diffusion membrane further comprises a permeability improving compound from the group hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, polyethylene glycole, polyvinyl pyrrolidone, fatty acids.

Claim 5

Dependent Claim 53 words

Pharmaceutical composition according to claim 1, characterized in that the diffusion membrane is a mixture of ethyl cellulose, and a copolymer of polyethyl methacrylate-methyl methacrylate-trimethyl ammonium ethylmethacrylate chloride in the weight relationship 80:20 to 20:80, whereby the weight relationship between the monomers of the copolymer is 63 to 65:31.7 to 32.3:2.5 to 5.

Claim 6

Dependent Claim 35 words

Pharmaceutical composition according to claims 1-4, characterized in that the active compound present in the core has a solubility in the pH range 1 to 8 which exceeds 0.5 to 1 g per 100 ml.

Claim 7

Dependent Claim 47 words

Pharmaceutical composition according to claim 5, characterized in that the active compound is quinidine sulphate, quinidine bisulphate, quinidine gluconate, quinidine hydrochloride, metoprolol tartrate, metoprolol succinate, metoprolol fumarate, furosemide, 5-amino salicylic acid, propranolol, alprenolol, or pharmaceutically acceptable salts thereof and/or other weak bases, weak acids, or salts thereof.

Claim 8

Dependent Claim 70 words

Pharmaceutical composition according to claims 1-6, characterized in that the core comprising the therapeutically active compound is a particle/granule having a diameter of 0.1 to 2.5 mm; that the first inner diffusion membrane is applied in an amount of at least 2.5 g per m 2 of particle area, and that the second layer is applied in an amount of at least 2.5 g per m 2 of particle area.

Claim 9

Dependent Claim 98 words

Process for the preparation of a pharmaceutical composition having an improved release of a therapeutically active compound, characterized in that a core comprising a therapeutically active compound is coated with an inner layer of a diffusion membrane comprising ethyl cellulose, and/or a copolymer of polyethyl methacrylate-methyl methacrylate-trimethylammonium ethyl methacrylate chloride by applying a solution containing said compound (-s), and is coated with a second layer of an anionic polymer, and/or fatty acid having a pk a of 4.5 to / by applying a solution containing said compound (-s), whereby said diffusion membrane optionally can contain permeability improving compounds.

Claim 10

Dependent Claim 98 words

Process for the preparation of a pharmaceutical composition having an improved release of a therapeutically active compound, characterized in that a core comprising a therapeutically active compound is coated with an inner layer of a diffusion membrane comprising ethyl cellulose, and/or a copolymer of polyethyl methacrylate-methyl methacrylate-trimethylammonium ethyl methacrylate chloride by applying a solution containing said compound (-s), and is coated with a second layer of an anionic polymer, and/or fatty acid having a pk a of 4.5 to / by applying a solution containing said compound (-s), whereby said diffusion membrane optionally can contain permeability improving compounds.

Claim 11

Dependent Claim 141 words

Pharmaceutical composition for an oral administration comprising a therapeutically active compound, characterized in that a part of the composition is a pharmaceutical composition according to claim 1 to 7, comprising a therapeutically active compound, a part is a pharmaceutical composition comprising the same therapeutical active compound, whereby this composition lacks a release preventing coating, and a part is a pharmaceutical composition comprising the same therapeutically active compound, whereby the latter composition is provided with a coating which gives a release of therapeutically active compound during 1 to 2 hrs, whereby this coating preferably is a diffusion membrane of the type which is the first layer of the pharmaceutical composition according to claims 1 to 7, whereby the different partial compositions are present in such an amount that a therapeutically acceptable blood plasma level is obtained after the administration of the composition.

Claim 12

Independent Claim 103 words

A method for the treatment of mammals, including man, by oral administration of a therapeutically active dose of a therapeutically active compound, characterized in that a core comprising a therapeutically active compound, on which core has been applied a first, inner diffusion membrane in the form of ethyl cellulose, and/or a copolymer of polyethyl methacrylate-methyl methacrylate-trimethylammonium ethyl methacrylate chloride, and a second layer of at least one anionic polymer, and/or fatty acid having a pk a of 4.5 to 7, is administered for the release of the therapeutically active compound in the lower part of the gastro-intestinal duct having a pH exceeding 4.5.

Claim 13

Independent Claim 103 words

A method for the treatment of mammals, including man, by oral administration of a therapeutically active dose of a therapeutically active compound, characterized in that a core comprising a therapeutically active compound, on which core has been applied a first, inner diffusion membrane in the form of ethyl cellulose, and/or a copolymer of polyethyl methacrylate-methyl methacrylate-trimethylammonium ethyl methacrylate chloride, and a second layer of at least one anionic polymer, and/or fatty acid having a pk a of 4.5 to 7, is administered for the release of the therapeutically active compound in the lower part of the gastro-intestinal duct having a pH exceeding 4.5.

Pharmaceutical composition

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