Active ingredient-containing floating forms comprising polyvinyl acetate and polyvinylpyrrolidone, their use and production

Claim 2

An oral dosage form comprising a) one or more active ingredients b) a formulated mixture of polyvinyl acetate and polyvinylpyrrolidone c) where appropriate other excipients customary for producing the dosage form, which floats on gastric fluid and displays delayed release of active ingredient, wherein the proportion of the formulated mixture of polyvinyl acetate and polyvinylpyrrolidone is between 20 and 70%, based on the total weight of the oral dosage form.

Claim 3

A dosage form as claimed in claim 1 , wherein the ratio of polyvinyl acetate to polyvinylpyrrolidone is from 6:4 to 9:1.

Claim 4

A dosage form as claimed in claim 1 , wherein the oral dosage form is a tablet, capsule or a coated tablet.

Claim 5

A dosage form as claimed in claim 1 , wherein the dosage form is a tablet.

Claim 6

A dosage form as claimed in claim 1 , wherein the release is adjusted by adding substances which are freely soluble in water, soluble in water, highly swelling or lipophilic.

Claim 7

A dosage form as claimed in claim 1 , wherein the friability is less than 3%.

Claim 8

A dosage form as claimed in claim 1 , wherein a water-soluble or water-insoluble, release-slowing coating is applied to the oral dosage form.

Claim 9

A dosage form as claimed in claim 5 , wherein the highly swelling substances which are soluble in water are selected from the group consisting of alginates, pectins, galactomannans, carrageenans, dextran, curdlan, pullulan, gellan, chitin, gelatin, xanthans, hemicelluloses, cellulose derivatives, starch derivatives, and derivatives thereof, and the lipophilic substances are selected from the group consisting of fatty alcohols, fatty acids, and lipophilic polymers.

Claim 10

A dosage form as claimed in claim 8 , wherein the highly swelling substances which are soluble in water are selected from the group consisting of methylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, carboxymethylcellulose, carboxymethyl starch, degraded starch, maltodextrins, polyacrylic acid, polymethacrylic acid, acrylic acid/methacrylic acid copolymers, polyvinyl alcohols, high molecular weight polyethylene glycols, polyoxyethylene/polyoxypropylene block copolymers, high molecular weight polyvinylpyrrolidones, and derivatives thereof.

Claim 11

A dosage form as claimed in claim 5 , wherein the substances which are soluble in water are selected from the group consisting of polyethylene glycols, polyvinylpyrrolidone and vinylpyrrolidone/vinyl acetate copolymers.

Claim 12

A dosage form as claimed in claim 5 , wherein the lipophilic substances are selected from the group consisting of stearyl alcohol, stearic acid, glycerides, fatty acid esters, fatty alcohol esters, ethylcellulose, cellulose acetate, acrylic ester/methacrylic ester copolymers, methacrylic acid/acrylic ester copolymers, cellulose acetate phthalate, cellulose acetate succinate, hydroxypropylmethylcellulose acetate phthalate, and hydroxypropylmethylcellulose acetate succinate.

Claim 13

A dosage form as claimed in claim 1 , which comprises as other excipients c) lubricants, binders, disintegrants, flow regulators, stabilizers, colorants or bulking agents.

Claim 14

A dosage form as claimed in claim 1 , which comprises as active ingredients a) food supplements or additives, vitamins, minerals or trace elements or active pharmaceutical ingredients.

Claim 15

A dosage form as claimed in claim 1 , which comprises as active ingredients a) active pharmaceutical ingredients.

Claim 16

A dosage form as claimed in claim 1 , wherein the active pharmaceutical ingredient is selected from the group consisting of benzodiazepines, antihypertensives, vitamins, cytostatics, anesthetics, neuroleptics, antidepressants, antibiotics, antimycotics, fungicides, chemotherapeutics, urologicals, platelet aggregation inhibitors, sulfonamides, spasmolytics, hormones, immunoglobulins, sera, thyroid therapeutics, psychopharmaceuticals, antiparkinson agents, other antihyperkinetics, ophthalmologicals, neuropathy products, calcium metabolism regulators, muscle relaxants, lipid-lowering agents, liver therapeutics, coronary agents, cardiac agents, immunotherapeutics, regulatory peptides, regulatory peptide inhibitors, hypnotics, sedatives, gynecologicals, antigout agents, fibrinolytics, enzyme products, transport proteins, enzyme inhibitors, emetics, perfusion promoters, diuretics, diagnostics, corticoids, cholinergics, biliary therapeutics, antiasthmatics, bronchiospasmolytics, beta-receptor blockers, calcium channel blockers, ACE inhibitors, arteriosclerosis remedies, antiinflammatory agents, anticoagulants, antihypotensives, antihypoglycemics, antifibrinolytics, antiepileptics, antiemetics, antidotes, antidiabetics, antiarrhythmics, antianemics, antiallergics, anthelmintics, analgesics, analeptics, aldosterone antagonists, and weight-reducing agents.

Claim 17

A dosage form as claimed in claim 1 , wherein two or more layers are present and differ in the content of active ingredient and formulated mixture of polyvinyl acetate and polyvinylpyrrolidone.

Claim 18

A dosage form as claimed in claim 1 , which is a press-coated tablet with a core with a very high active ingredient content.

Claim 19

A process for producing oral dosage forms as claimed in claim 1 , which comprises tableting an initial mixture of the dosage form components using a pressure of less than 100 MPa.

Claim 20

A process for producing oral dosage forms as claimed in claim 18 , wherein the initial mixture is tableted directly or the initial mixture or a part thereof is wet-granulated or dry-compacted before the tableting.

Claim 21

A drug product for delayed release of active ingredient, which is an oral dosage form as claimed in claim 1 .

Claim 22

A process for producing drug products with delayed release of active ingredient for treating diseases, comprising incorporating the active ingredient into the oral dosage form as claimed in claim 1 .

Claim 23

The process as claimed in claim 21 , wherein the active ingredient is selected from the group consisting of food supplements, food additives, vitamins, minerals, trace elements, and active pharmaceutical ingredients.