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US4578264A Expired / Lapsed US ⏱️ 0.0 years remaining

Retard form of pharmaceuticals with insoluble porous diffusion coatings

Assignee: Boehringer Ingelheim GmbH
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Filing: 1984-04-27
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Granted: 1986-03-25
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Expires: 2004-04-27
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Abstract

Abstract This invention relates to a pharmaceutical dosage unit composition consisting essentially of a gelatin capsule containing (1) a disintegrating core comprising clonidine, said disintegrating core having a readily water-soluble coating, and (2) a plurality of non-disintegrating cores comprising clonidine, said non-disintegrating cores having a coating consisting of from 20 to 90 percent by weight of a water-insoluble film former and from 10 to 80 percent by weight of a water-soluble polymer, the diameter of each of the disintegrating and non-disintegrating cores being at least about 5 mm.

Inventors

  • 👤 Herbert Stricker
  • 👤 Bernhard Freund
  • 👤 Heribert Harwalik
  • 👤 Karl L. Rominger
  • 👤 Siegfried Darda
  • 👤 Volkmar Haselbarth
  • 👤 Dietrich Arndts
  • 👤 Wolf D. Bechtel
  • 👤 Gerhard Bozler
  • 👤 Rolf Brickl
  • 👤 Peter Gruber

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 19:10
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/55; A61K9/00; A61K9/20; A61K9/28; A61K9/2806; A61K9/2833; A61K9/2853; A61K9/286; A61K9/2866; A61K9/48; A61K9/4808

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 83 words
A pharmaceutical dosage unit composition consisting essentially of a gelatin capsule containing (1) a disintegrating core comprising clonidine, said disintegrating core having a readily water-soluble coating, and (2) a plurality of non-disintegrating cores comprising clonidine, said non-disintegrating cores having a coating consisting of from 20 to 90 percent by weight of a water-insoluble film former and from 10 to 80 percent by weight of a water-soluble polymer, the diameter of each of the disintegrating and non-disintegrating cores being at least about 5 mm.
Claim 2
Dependent Claim 83 words
A pharmaceutical dosage unit composition consisting essentially of a gelatin capsule containing (1) a disintegrating core comprising clonidine, said disintegrating core having a readily water-soluble coating, and (2) a plurality of non-disintegrating cores comprising clonidine, said non-disintegrating cores having a coating consisting of from 20 to 90 percent by weight of a water-insoluble film former and from 10 to 80 percent by weight of a water-soluble polymer, the diameter of each of the disintegrating and non-disintegrating cores being at least about 5 mm.
Claim 3
Dependent Claim 23 words
The dosage unit composition of claim 1, wherein the clonidine is present in a total amount of from about 0.1 to 1.5 mgm.
Claim 4
Dependent Claim 41 words
The dosage unit composition of claim 1, wherein the capsule also contains a disintegrating core comprising chlorothalidone or hydrochlorothiazide, as a second active substance, said core having a readily soluble water-soluble coating and having a diameter of at least 5 mm.
Claim 5
Dependent Claim 40 words
The dosage unit composition of claim 3, wherein the second active substance is present in a total amount of from about 10 to 50 mgm and the clonidine is present in an amount of from about 0.05 to 1.5 mgm.
Claim 6
Dependent Claim 28 words
The dosage unit composition of claim 1, wherein the readily water-soluble coating comprises 90 percent by weight of hydroxypropylmethyl cellulose and 10 percent by weight of polyethylene glycol.
Claim 7
Dependent Claim 30 words
The dosage unit composition of claim 1, wherein the water-insoluble film former is selected from the group consisting of ethyl cellulose and polymeric lacquer substances based upon acrylate or methyacrylate.
Claim 8
Dependent Claim 15 words
The dosage unit composition of claim 6, wherein the water-insoluble film former is ethyl cellulose.
Claim 9
Dependent Claim 24 words
The dosage unit composition of claim 1, wherein the water-soluble polymer is selected from the group consisting of polyethylene glycol, methyl cellulose, and polyvinylpyrrolidone.
Claim 10
Dependent Claim 26 words
The dosage unit composition of claim 1, wherein the coating of the non-disintegrating cores also contains up to 80 percent by weight of an acid-insoluble polymer.
Claim 11
Dependent Claim 34 words
The dosage unit composition of claim 9, wherein the acid-insoluble polymer is selected from the group consisting of cellulose acetate phthalate, hydroxypropylmethyl cellulose phthalate, and partially esterified polymethacrylic acid optionally containing a softening agent.
Claim 12
Dependent Claim 14 words
The dosage unit composition of claim 1, wherein the cores are tablets or pellets.
Claim 13
Dependent Claim 20 words
The dosage unit composition of claim 1, wherein the cores have a diameter of from about 5 to 6.2 mm.
Claim 14
Dependent Claim 31 words
A method for the treatment of cardiovascular disorders in a host in need of such treatment which comprises administering to said host an effective amount of a composition of claim 1.

References Cited (Backward Citations)

GB908282A Cited
GB1469133A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1989-03-24 1989-09-23 1990-03-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1993-03-24 1993-09-23 1994-03-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1997-03-24 1997-09-23 1998-03-25 $7700.00 Window Closed / Lapsed

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