US4361546A
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: 1981-06-15
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Granted: 1982-11-30
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Expires: 2001-06-15
Abstract
Abstract A pharmaceutical dosage unit retard form having a constant, pH-independent release rate of active ingredient, consisting of a core comprising an active ingredient, and a semi-permeable diffusion coating over the core, were the coating consists of a water-insoluble film-former, a water-soluble polymer and eventually an acid-insoluble polymer incorporated therein.
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
2026-10-25 01:22
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: 26
Claim 1
Independent Claim
121 words
A pharmaceutical dosage unit composition consisting essentially of a gelatin capsule containing (1) a disintegrating core comprising (i) dipyridamole or an acid addition salt thereof and (ii) an acid substance in an amount sufficient to make the dipyridamole water-soluble and having a readily water-soluble coating, and (2) a plurality of non-disintegrating cores comprising (i) dipyridamole or an acid addition salt thereof and (ii) an acid substance in an amount sufficient to make the dipyridamole water-soluble and 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
121 words
A pharmaceutical dosage unit composition consisting essentially of a gelatin capsule containing (1) a disintegrating core comprising (i) dipyridamole or an acid addition salt thereof and (ii) an acid substance in an amount sufficient to make the dipyridamole water-soluble and having a readily water-soluble coating, and (2) a plurality of non-disintegrating cores comprising (i) dipyridamole or an acid addition salt thereof and (ii) an acid substance in an amount sufficient to make the dipyridamole water-soluble and 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 acid substance is selected from the group consisting of citric acid and tartaric acid.
Claim 4
Dependent Claim
22 words
The dosage unit composition of claim 1, wherein the molar ratio of dipyridamole to acid substance is from about 1:1 to 1:3.
Claim 5
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 6
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 methacrylate.
Claim 7
Dependent Claim
15 words
The dosage unit composition of claim 5, wherein the water-insoluble film former is ethyl cellulose.
Claim 8
Dependent Claim
25 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 polyvinyl pyrrolidone.
Claim 9
Dependent Claim
26 words
The dosage unit composition of claim 1, wherein the coating on the non-disintegrating cores also contains up to 80 percent by weight of an acid-insoluble polymer.
Claim 10
Dependent Claim
34 words
The dosage unit composition of claim 8, 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 11
Dependent Claim
14 words
The dosage unit composition of claim 1, wherein the cores are tablets or pellets.
Claim 12
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 13
Dependent Claim
27 words
The dosage unit composition of claim 1, wherein the dipyridamole or acid addition salt thereof is present in a total amount of from 150 to 400 mgm.
Claim 14
Dependent Claim
153 words
The dosage unit composition of claim 1 consisting essentially of a gelatin capsule containing (1) a disintegrating tablet comprising dipyridamole and an acid substance selected from the group consisting of citric acid and tartaric acid, the molar ratio of dipyridamole to acid substance being from about 1:1 to 1:3, said tablet having a coating consisting of 90 percent by weight of hydroxypropylmethyl cellulose and 10 percent by weight of polyethylene glycol, and (2) five non-disintegrating tablets comprising dipyridamole and an acid substance selected from the group consisting of citric acid and tartaric acid, the molar ratio of dipyridamole to acid substance being from about 1:1 to 1:3, each of said non-disintegrating tablets having a coating consisting of from about 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 tablets being about 6.2 mm.
Claim 15
Dependent Claim
32 words
A method for the treatment of cardiovascular disorders in a host in need of such treatment which comprises administering to said host a cardiovascularly effective amount of a composition of claim 1.
Claim 16
Dependent Claim
21 words
The method of claim 14, wherein the acid substance is selected from the group consisting of citric acid and tartaric acid.
Claim 17
Dependent Claim
20 words
The method of claim 14, wherein the molar ratio of dipyridamole to acid substance is from about 1:1 to 1:3.
Claim 18
Dependent Claim
26 words
The method of claim 14, wherein the readily water-soluble coating comprises 90 percent by weight of hydroxypropylmethyl cellulose and 10 percent by weight of polyethylene glycol.
Claim 19
Dependent Claim
28 words
The method of claim 14, wherein the water-insoluble film former is selected from the group consisting of ethyl cellulose and polymeric lacquer substances based upon acrylate or methacrylate.
Claim 20
Dependent Claim
13 words
The method of claim 18, wherein the water-insoluble film former is ethyl cellulose.
Claim 21
Dependent Claim
23 words
The method of claim 14, wherein the water-soluble polymer is selected from the group consisting of polyethylene glycol, methyl cellulose, and polyvinyl pyrrolidone.
Claim 22
Dependent Claim
24 words
The method of claim 14, wherein the coating on the non-disintegrating cores also contains up to 80 percent by weight of an acid-insoluble polymer.
Claim 23
Dependent Claim
32 words
The method of claim 21, 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 24
Dependent Claim
18 words
The method of claim 14, wherein the cores have a diameter of from about 5 to 6.2 mm.
Claim 25
Dependent Claim
25 words
The method of claim 14, wherein the dipyridamole or acid addition salt thereof is present in a total amount of from 150 to 400 mgm.
Claim 26
Dependent Claim
156 words
The method of claim 14, wherein the dosage unit composition consists essentially of a gelatin capsule containing (1) a disintegrating tablet comprising dipyridamole and an acid substance selected from the group consisting of citric acid and tartaric acid, the molar ratio of dipyridamole to acid substance being from about 1:1 to 1:3, and tablet having a coating consisting of 90 percent by weight of hydroxypropylmethyl cellulose and 10 percent by weight of polyethylene glycol, and (2) five non-disintegrating tablets comprising dipyridamole and an acid substance selected from the group consisting of citric acid and tartaric acid, the molar ratio of dipyridamole to acid substance being from about 1:1 to 1:3, each of said non-disintegrating tablets having a coating consisting of from about 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 tablets being about 6.2 mm.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-11-29 | 1986-05-31 | 1986-11-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-11-29 | 1990-05-31 | 1990-11-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-11-29 | 1994-05-31 | 1994-11-30 | $7700.00 | Window Closed / Lapsed |