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US4083949A Expired / Lapsed US ⏱️ 0.0 years remaining

New oral form of medicament and a method for producing it

Assignee: Takeda GmbH
•
Filing: 1974-07-08
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Granted: 1978-04-11
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Expires: 1994-07-08
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Abstract

Abstract An oral form of medicament releases active substance in the gastrointestinal tract at a constant rate.

Inventors

  • 👤 Gerald Benedikt

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-22 22:51
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5073; A61K9/5078

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 184 words
A therapeutically-useful and pharmacologically-acceptable oral depot medicament form comprising substantially uniformly-sized spheroidal medicament particals, each of which is provided with a dialysis membrane and has a diameter of between 0.1 and 2 millimeters, the dialysis membrane having a film-forming component which comprises (a) from 15 to 70 percent by weight of a cellulose ether, selected from the group consisting of methyl cellulose, ethyl cellulose and propyl cellulose, which is insoluble in the pH range of the gastrointestinal tract, which is not enzymatically degraded, which has an alkoxy-group content of from 43 to 50 percent by weight, and which has a viscosity of from about 7 to 100 centipoises in a 5 percent by weight toluene-ethanol mixture (80:20 parts by weight) at 25° C and (b) from 85 to 30 percent by weight of an organic-compound component which is substantially only soluble in the alkaline pH range of the intestinal tract, which contains from 5 to 40 percent by weight of free carboxyl groups, and which comprises at least one organic compound selected from the group consisting of palmitic acid, myristic acid and stearic acid.
Claim 2
Dependent Claim 184 words
A therapeutically-useful and pharmacologically-acceptable oral depot medicament form comprising substantially uniformly-sized spheroidal medicament particals, each of which is provided with a dialysis membrane and has a diameter of between 0.1 and 2 millimeters, the dialysis membrane having a film-forming component which comprises (a) from 15 to 70 percent by weight of a cellulose ether, selected from the group consisting of methyl cellulose, ethyl cellulose and propyl cellulose, which is insoluble in the pH range of the gastrointestinal tract, which is not enzymatically degraded, which has an alkoxy-group content of from 43 to 50 percent by weight, and which has a viscosity of from about 7 to 100 centipoises in a 5 percent by weight toluene-ethanol mixture (80:20 parts by weight) at 25° C and (b) from 85 to 30 percent by weight of an organic-compound component which is substantially only soluble in the alkaline pH range of the intestinal tract, which contains from 5 to 40 percent by weight of free carboxyl groups, and which comprises at least one organic compound selected from the group consisting of palmitic acid, myristic acid and stearic acid.
Claim 3
Dependent Claim 20 words
A therapeutically-useful and pharmacologically-acceptable oral depot medicament form according to claim 1 wherein the cellulose ether (a) is ethyl cellulose.
Claim 4
Dependent Claim 13 words
An oral depot medicament form according to claim 1 comprising readily water-soluble medicament.
Claim 5
Dependent Claim 22 words
An oral depot medicament according to claim 1 comprising medicament which is sparingly soluble in neutral to alkaline parts of the intestine.
Claim 6
Dependent Claim 57 words
A medicament form according to claim 1 containing active ingredient which (a) is a nitrogen-containing base with a pK B -value of from 5 to 14 or a salt of such base or (b) has a solubility quotient of from 2:1 to 1500:1 based on its solubility in the stomach divided by that in the intestinal tract.
Claim 7
Dependent Claim 21 words
A medicament form according to claim 1, the spheroidal particles of which have a diameter of from 0.8 to 1.6 millimeters.
Claim 8
Dependent Claim 20 words
A medicament form according to claim 1, the spheroidal particles of which have a diameter of up to 1 millimeter.
Claim 9
Dependent Claim 11 words
A medicament form according to claim 1 in unit dosage form.
Claim 10
Dependent Claim 10 words
A medicament form according to claim 8 in capsule form.
Claim 11
Dependent Claim 20 words
A tableted therapeutically-useful and pharmacologically-acceptable oral depot medicament form wherein the oral depot medicament form is that of claim 1.
Claim 12
Dependent Claim 23 words
A therapeutically-useful and pharmacologically-acceptable oral depot medicament form according to claim 1 and wherein the dialysis membrane consists essentially of (a) and (b).
Claim 13
Dependent Claim 22 words
A therapeutically-useful and pharmacologically-acceptable oral depot medicament form according to claim 2 wherein component (b) of the dialysis membrane comprises stearic acid.
Claim 14
Dependent Claim 22 words
A therapeutically-useful and pharmacologically-acceptable oral depot medicament form according to claim 2 wherein component (b) of the dialysis membrane comprises palmitic acid.
Claim 15
Dependent Claim 22 words
A therapeutically-useful and pharmacologically-acceptable oral depot medicament form according to claim 2 wherein component (b) of the dialysis membrane comprises myristic acid.
Claim 16
Dependent Claim 56 words
A therapeutically-useful and pharmacologically-acceptable oral depot medicament form according to claim 1 and wherein the dialysis membrane film-forming component further comprises anionic polymerizate of methacrylic acid and methacrylic acid ester which is soluble in the neutral pH range above 6 and which has a free carboxylic-acid-group content ranging from about 20 to 40 percent by weight.

References Cited (Backward Citations)

US2921883A Cited
US3247066A Cited
US3673084A Cited
US3567809A Cited
US3538214A Cited
US3593855A Cited
US3780147A Cited
US3648845A Cited
US3835221A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-04-10 1981-10-10 1982-04-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-04-10 1985-10-10 1986-04-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-04-10 1989-10-10 1990-04-11 $7700.00 Window Closed / Lapsed

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