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US4017598A Expired / Lapsed US ⏱️ 0.0 years remaining

Preparation of readily disintegrable tablets

Assignee: Shin-Etsu Chemical Co Ltd
•
Filing: 1975-04-22
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Granted: 1977-04-12
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Expires: 1995-04-22
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Abstract

Abstract Methylcellulose with or without the addition of medically active ingredients and other additives is first granulated by a known method into granules of appropriate size and then the granules are blended with a disintegrator and compressed into tablets. The tablets obtained by the method have sufficient hardness and very short disintegration time when taken into the human body in comparison with the poor disintegrability of tablets directly shaped from powdery methylcellulose or a methylcellulose-based mixture of active ingredients. The method is useful for tableting some medicinals of poor tabletability, such as, pancreatin which require large amounts of a binder to be successfully shaped into tablets. Tablets of methylcellulose prepared in accordance with the method can find use as a non-caloried food.

Inventors

  • 👤 Shigeru Ohno
  • 👤 Noboru Hoshi
  • 👤 Fujio Sekigawa

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 20:12
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/205; A61K9/2054

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 146 words
A method for the preparation of readily disintegrable tablets which comprises the steps of (a) granulating powdery methylcellulose wetted with a mixed solvent of water and and an alcohol selected from the group consisting of methanol, ethanol and propanol in a ratio of from 9:1 to 1:9 by weight into granules, (b) admixing a disintegrator selected from the group consisting of a microcrystalline cellulose, calcium salt of carboxymethylcellulose, methylcellulose with the degree of substitution in the range of from 0.1 to 1.2, hydroxypropylcellulose with the molar substitution in the range of from 0.1 to 1.2 and hydroxypropylmethylcellulose with the degree of molar substitution for the methoxy groups and hydroxypropoxy groups in the range of from 0.1 to 1.2 with said granules in an amount of from 3% to 200% by weight based on said granules to form a blend, and (c) shaping said blend into tablets.
Claim 2
Independent Claim 146 words
A method for the preparation of readily disintegrable tablets which comprises the steps of (a) granulating powdery methylcellulose wetted with a mixed solvent of water and and an alcohol selected from the group consisting of methanol, ethanol and propanol in a ratio of from 9:1 to 1:9 by weight into granules, (b) admixing a disintegrator selected from the group consisting of a microcrystalline cellulose, calcium salt of carboxymethylcellulose, methylcellulose with the degree of substitution in the range of from 0.1 to 1.2, hydroxypropylcellulose with the molar substitution in the range of from 0.1 to 1.2 and hydroxypropylmethylcellulose with the degree of molar substitution for the methoxy groups and hydroxypropoxy groups in the range of from 0.1 to 1.2 with said granules in an amount of from 3% to 200% by weight based on said granules to form a blend, and (c) shaping said blend into tablets.
Claim 3
Dependent Claim 31 words
The method as claimed in claim 1, wherein said mixed solvent is employed in an amount of from 20% to 80% by weight based on the weight of said powdery methylcellulose.
Claim 4
Independent Claim 161 words
A method for the preparation of readily disintegrable tablets which comprises the steps of (a) granulating a material selected from the group consisting of powdery methylcellulose and mixtures of methylcellulose with medically active ingredients wetted with a mixed solvent of water and an alcohol selected from the group consisting of methanol, ethanol and propanol in a ratio of from 9:1 to 1:9 by weight into granules, (b) admixing a disintegrator selected from the group consisting of a microcrystalline cellulose, calcium salt of carboxymethylcellulose, methylcellulose with the degree of substitution in the range of from 0.1 to 1.2, hydroxypropylcellulose with the molar substitution in the range of from 0.1 to 1.2 and hydroxypropylmethylcellulose with the degree of molar substitution for the methoxy groups and hydroxypropoxy groups in the range of from 0.1 to 1.2 with said granules in an amount of from 3% to 200% by weight based on said granules to form a blend, and (c) shaping said blend into tablets.
Claim 5
Independent Claim 161 words
A method for the preparation of readily disintegrable tablets which comprises the steps of (a) granulating a material selected from the group consisting of powdery methylcellulose and mixtures of methylcellulose with medically active ingredients wetted with a mixed solvent of water and an alcohol selected from the group consisting of methanol, ethanol and propanol in a ratio of from 9:1 to 1:9 by weight into granules, (b) admixing a disintegrator selected from the group consisting of a microcrystalline cellulose, calcium salt of carboxymethylcellulose, methylcellulose with the degree of substitution in the range of from 0.1 to 1.2, hydroxypropylcellulose with the molar substitution in the range of from 0.1 to 1.2 and hydroxypropylmethylcellulose with the degree of molar substitution for the methoxy groups and hydroxypropoxy groups in the range of from 0.1 to 1.2 with said granules in an amount of from 3% to 200% by weight based on said granules to form a blend, and (c) shaping said blend into tablets.
Claim 6
Dependent Claim 42 words
The method as claimed in claim 3, wherein said mixed solvent is employed in an amount of from 20% to 80% by weight based on the weight of said powdery methylcellulose or said mixed powder of methylcellulose and a medically active ingredient.
Claim 7
Dependent Claim 49 words
The method as claimed in claim 1, wherein the size of said granules is such that all of said granules pass through a sieve with an opening of 2,000 μm and less than 5% by weight of said granules pass through a sieve with an opening of 177 μm.
Claim 8
Dependent Claim 27 words
The method as claimed in claim 1, wherein said methylcellulose has a content of the methoxy groups in the range of from 20% to 32% by weight.
Claim 9
Dependent Claim 34 words
The method as claimed in claim 1, wherein the viscosity of the 2% by weight aqueous solution of said methylcellulose is in the range of from 5 centipoise to 10,000 centipoise at 20° C.
Claim 10
Dependent Claim 50 words
The method as claimed in claim 3, wherein said mixed powder of methylcellulose and a medically active ingredient is a mixture of less than 300 parts by weight of said medically active ingredient and 100 parts by weight of said methylcellulose when said medically active ingredient is in powder form.
Claim 11
Dependent Claim 50 words
The method as claimed in claim 3, wherein said mixed powder of methylcellulose and a medically active ingredient is a mixture of less than 50 parts by weight of said medically active ingredient and 100 parts by weight of said methylcellulose when said medically active ingredient is in liquid form.

References Cited (Backward Citations)

US2883327A Cited
US3079303A Cited
US3065143A Cited
US3133863A Cited
US3266992A Cited
US3852421A Cited
US3725556A Cited
US3907983A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-04-11 1980-10-11 1981-04-12 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-04-11 1984-10-11 1985-04-12 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-04-11 1988-10-11 1989-04-12 $7700.00 Window Closed / Lapsed

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