US4427648A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Dipyridamole-containing pharmaceutical form
Assignee: Boehringer Ingelheim Pharma GmbH and Co KG
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Filing: 1982-06-17
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Granted: 1984-01-24
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Expires: 2002-06-17
Abstract
Abstract This invention relates to vehicles for the administration of dipyridamole. More specifically, this invention relates to a method of treating cardiovascular disorders in a host in need of such treatment which comprises administering to said host a cardiovascularly effective amount of a composition comprised of (i) dipyridamole or an acid addition salt thereof and (ii) at least one pharmacologically acceptable acid or acid substance, the total amount of acid from acid addition salt present and acid or acid substance being in a ratio of at least about 5 acid equivalents to 1 mol of dipyridamole, preferably in the form of particles having particle sizes of from about 0.1 to 2.0 mm.
Inventors
- 👤 Rolf Brickl
- 👤 Peter Gruber
- 👤 Gottfried Schepky
- 👤 Gerhard Bozler
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 23:48
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/14; A61K9/16; A61K9/1605; A61K9/1617; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K9/2004; A61K9/2013; A61K9/48; A61K9/50; A61K9/5073; A61K9/5078; A61P; A61P9/00; A61P9/08; A61P9/10
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
81 words
A method of treating cardiovascular disorders in a host in need of such treatment which comprises administering to said host a cardiovascularly effective amount of an uncoated composition consisting essentially of (i) dipyridamole or an acid addition salt thereof and (ii) at least one pharmacologically acceptable acid or acid substance, the total amount of acid from acid addition salt present and acid or acid substance being in a ratio of at least about 5 acid equivalents to 1 mol of dipyridamole.
Claim 2
Independent Claim
81 words
A method of treating cardiovascular disorders in a host in need of such treatment which comprises administering to said host a cardiovascularly effective amount of an uncoated composition consisting essentially of (i) dipyridamole or an acid addition salt thereof and (ii) at least one pharmacologically acceptable acid or acid substance, the total amount of acid from acid addition salt present and acid or acid substance being in a ratio of at least about 5 acid equivalents to 1 mol of dipyridamole.
Claim 3
Dependent Claim
38 words
The method of claim 1, wherein the total amount of acid from acid addition salt present and acid or acid substance is in a ratio of from about 10 to 30 acid equivalents to 1 mol of dipyridamole.
Claim 4
Dependent Claim
66 words
The method of claim 1, wherein the pharmacologically acceptable acid or acid substance is selected from the group consisting of tartaric acid, citric acid, fumaric acid, succinic acid, malic acid, ascorbic acid, adipic acid, sodium or potassium salts of said acids, sodium or potassium hydrogen sulfate, betaine hydrochloride, anhydrides of succinic or glutaric acid which hydrolyse in water to form acids, D-glucuronic acid-γ-lactone, and mixtures thereof.
Claim 5
Dependent Claim
18 words
The method of claim 1 or 2, wherein the pharmacologically acceptable acid or acid substance is fumaric acid.
Claim 6
Dependent Claim
14 words
The method of claim 1, wherein the composition is in the form of granules.
Claim 7
Dependent Claim
18 words
The method of claim 5, wherein the granules have particle sizes of from about 0.1 to 2.0 mm.
Claim 8
Dependent Claim
18 words
The method of claim 6, wherein the granules have particle sizes of from about 0.25 to 1.25 mm.
Claim 9
Dependent Claim
14 words
The method of claim 5, wherein the granules are contained in hard gelatin capsules.
Claim 10
Dependent Claim
14 words
The method of claim 1, wherein the composition is in the form of pellets.
Claim 11
Dependent Claim
17 words
The method of claim 9, wherein the pellets have diameters of from about 0.1 to 2.0 mm.
Claim 12
Dependent Claim
17 words
The method of claim 10, wherein the pellets have diameters of from about 0.5 to 1.5 mm.
Claim 13
Dependent Claim
14 words
The method of claim 9, wherein the pellets are contained in hard gelatin capsules.
Claim 14
Dependent Claim
17 words
The method of claim 1, wherein the composition is in the form of tablets or tablet cores.
Claim 15
Dependent Claim
13 words
The method of claim 1, wherein the composition also comprises conventional pharmacological additives.
Claim 16
Dependent Claim
24 words
The method of claim 14, wherein the additives are selected from the group consisting of water-soluble binders, mucilaginous excipients, water-repellent excipients, and mixtures thereof.
Claim 17
Dependent Claim
26 words
The method of claim 15, wherein the additives are selected from the group consisting of methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxypropyl methylcellulose, polyacrylic acids, fats, and mixtures thereof.
Claim 18
Dependent Claim
42 words
The method of claim 1, wherein the composition is in the form of particles having a coating comprised of a lacquer which permits the release of at least 90% of the dipyridamole in the gastrointestinal tract over a period of two hours.
Claim 19
Dependent Claim
74 words
The method of claim 1, wherein the composition comprises tablet cores prepared by compressing granules consisting of dipyridamole or an acid addition salt thereof, acid or acid substance, lubricant, and other conventional additives to form uncoated tablet cores and then coating said uncoated tablet cores with a flavor-masking coating or a lacquer coating which permits the release of at least 90% of the dipyridamole in the gastrointestinal tract over a period of two hours.
Claim 20
Dependent Claim
90 words
The method of claim 1, wherein the composition comprises cores prepared by (a) moist or dry granulation of (i) dipyridamole or an acid addition salt thereof and (ii) acid or acid substance to form a granulate; (b) addition of further, conventional excipients to said granulate; (c) compression of said granulate to form uncoated cores; and (d) coating of said uncoated cores with a flavor-masking coating or a lacquer coating which permits the release of at least 90% of the dipyridamole in the gastrointestinal tract over a period of two hours.
Claim 21
Dependent Claim
94 words
The method of claim 1, wherein the composition comprises cores prepared by (a) moist or dry granulation of (i) dipyridamole or an acid addition salt thereof and (ii) conventional excipients to form a granulate; (b) addition of one or more acids or acid substances and lubricant to said granulate; (c) compression of said granulate to form uncoated cores; and (d) coating of said uncoated cores with a flavor-masking coating or a lacquer coating which permits the release of at least 90% of the dipyridamole in the gastrointestinal tract over a period of two hours.
Claim 22
Dependent Claim
15 words
The method of claim 18, 19, or 20, wherein the coating is a flavor-masking coating.
Claim 23
Dependent Claim
32 words
The method of claim 18, 19, or 20, wherein the coating is a lacquer coating which permits the release of the dipyridamole in the gastrointestinal tract over a period of two hours.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-01-23 | 1987-07-25 | 1988-01-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-01-23 | 1991-07-25 | 1992-01-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-01-23 | 1995-07-25 | 1996-01-24 | $7700.00 | Window Closed / Lapsed |