PROCESS FOR PRODUCING SOLID ORAL DOSAGE FORMS WITH SUSTAINED RELEASE OF ACTIVE INGREDIENT
The present invention relates to a process for producing solid oral dosage forms with sustained release of active ingredient, comprising at least one active ingredient, a preformulated mixture of polyvinyl acetate and polyvinylpyrrolidone, where appropriate, water-soluble polymers or lipophilic additives and, where appropriate, other conventional excipients, wherein this mixture or parts of this mixture are granulated by heating to from 40° C. to 130° C., and the granules are, after admixture with conventional excipients, subsequently tabletted.
1 .- 16 . (canceled)
17 . An oral dosage form comprising
a) a formulated mixture of polyvinyl acetate and polyvinylpyrrolidone, wherein the polyvinylpyrrolidone is finely dispersed in the polyvinyl acetate,
b) at least one active ingredients
c) optionally where appropriate water-soluble polymers or low or high molecular weight lipophilic additives, and
d) optionally excipients, wherein the mixture of a) to d) or a) to c) or a) and b) and d) or a) and b) is granulated by heating to from 40° C. to 130° C.
18 . An oral dosage form as claimed in claim 17 , which comprises as active ingredients food supplements or additives, vitamins, minerals or trace elements or active pharmaceutical ingredients.
19 . An oral dosage form as claimed in claim 17 , which comprises active pharmaceutical ingredients as active ingredients.
20 . An oral dosage form as claimed in claim 19 , wherein the active pharmaceutical ingredient is selected from the group 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 and other antihyperkinetics, ophthalmologicals, neuropathy products, calcium metabolism regulators, muscle relaxants, lipid-lowering agents, liver therapeutics, coronary agents, cardiac agents, immunotherapeutics, regulatory peptides and their inhibitors, hypnotics, sedatives, gynecologicals, antigout agents, fibrinolytics, enzyme products and transport proteins, enzyme inhibitors, emetics, perfusion promoters, diuretics, diagnostics, corticoids, cholinergics, biliary therapeutics, antiasthmatics, bronchospasmolytics, 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, weight-reducing agents.
21 . An oral dosage form as claimed in claim 17 , which is used to produce compressed tablets.
22 . A drug product with delayed release of active ingredient, which is an oral dosage form as claimed in claim 17 .
23 . A drug product for delayed release of active ingredient, which is an oral dosage form as claimed in claim 17 which has been produced by compression.
24 .- 25 . (canceled)
26 . An oral dosage form as claimed in claim 17 which comprises water or solvent in amounts of less than 5% to increase surface moisture.
27 . An oral dosage form as claimed in claim 17 , wherein the polyvinyl acetate to polyvinylpyrrolidone ratio is from 6:4 to 9:1.
28 . An oral dosage form as claimed in claim 17 , wherein the active ingredient to component (c) ratio employed in the combination is from 5:95 to 85:15.
29 . A method of delaying the release of at least one active ingredient which comprises producing the oral dosage form of claim 17 wherein the at least one active ingrdient comprises food supplements or additives, vitamins, minerals or trace elements.
30 . An oral dosage form comprising
a) a formulated mixture of polyvinyl acetate and polyvinylpyrrolidone which acts as a binder and a matrix former, and wherein the polyvinylpyrrolidone has a molecular weight of from 20,000 to 1,000,000, and the polyvinylpyrrolidone is finely dispersed in the polyvinyl acetate,
b) at least one active ingredient,
c) optionally water-soluble polymers or low or high molecular weight lipophilic additives, and
d) optionally excipients,
which is obtained by a process which comprises granulating a mixture of a) to d) or a) to c) or a) and b) and d) or a) and b) by heating to a temperature of from 40° C. to 130° C. in the absence of solvents.
31 . An oral dosage form as claimed in claim 30 , which comprises as active ingredients food supplements or additives, vitamins, minerals or trace elements or active pharmaceutical ingredients.
32 . An oral dosage form as claimed in claim 30 , which comprises active pharmaceutical ingredients as active ingredients.
33 . An oral dosage form as claimed in claim 32 , wherein the active pharmaceutical ingredient is selected from the group 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 and other antihyperkinetics, ophthalmologicals, neuropathy products, calcium metabolism regulators, muscle relaxants, lipid-lowering agents, liver therapeutics, coronary agents, cardiac agents, immunotherapeutics, regulatory peptides and their inhibitors, hypnotics, sedatives, gynecologicals, antigout agents, fibrinolytics, enzyme products and transport proteins, enzyme inhibitors, emetics, perfusion promoters, diuretics, diagnostics, corticoids, cholinergics, biliary therapeutics, antiasthmatics, bronchospasmolytics, 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, weight-reducing agents.
34 . An oral dosage form as claimed in claim 30 which comprises water or solvent in amounts of less than 5% to increase surface moisture.
35 . An oral dosage form as claimed in claim 30 , wherein the polyvinyl acetate to polyvinylpyrrolidone ratio is from 6:4 to 9:1.
36 . An oral dosage form as claimed in claim 30 , wherein the active ingredient to component (c) ratio employed in the combination is from 5:95 to 85:15.
37 . An oral dosage form as claimed in claim 30 , wherein polyvinyl acetate and polyvinylpyrrolidone each have a molecular weight of from 20,000 to 1,000,000.
38 . A method of delaying the release of at least one active ingredient which comprises producing the oral dosage form of claim 30 wherein the at least one active ingrdient comprises food supplements or additives, vitamins, minerals or trace elements.