Oral mopidamol preparation

• US 4,596,705 A
• Filed: 10/07/1983
• Issued: 06/24/1986
• Est. Priority Date: 10/09/1982
• Status: Expired due to Term

• Current Assignee: Dr. Karl Thomae GmbH (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Dr. Karl Thomae GmbH (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Gruber, Peter, Schmid, Jochen, Schepky, Gottfried, Brickl, Rolf, Springmeier, Ursula
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/539,998
• Time in Patent Office: 991 Days
• Field of Search: 424/14, 424/16, 424/19-22, 424/31-38
• US Class Current: 424/468
• CPC Class Codes: A61K 31/505 Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/4841 Filling excipients; Inactive ingredients
• CPC Class Codes: A61K 9/5078 with drug-free core
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

Abstract

This invention relates to vehicles for the administration of mopidamol. More specifically, this invention relates to a method of treating cardiovascular disorders, malignancy, or thrombosis in a host in need of such treatment which comprises administering to said host a cardiovascularly, antimetastic, or antithrombotic effective amount of a composition comprised of (i) mopidamol 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 1 acid equivalent to 1 mol of mopidamol.

Claims

1. A composition which comprises (i) mopidamol 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 1 acid equivalent to 1 mol of mopidamol.

2. The composition 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 1 to 8 acid equivalents to 1 mol of mopidamol.

3. The composition 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.

4. The method of claim 1, wherein the pharmacologically acceptable acid or acid substance is fumaric acid.

5. The composition of claim 1, wherein the composition is in the form of tablets or tablet cores.

6. The composition of claim 1, wherein the composition also comprises conventional pharmacological additives.

7. The composition of claim 6, wherein the additives are selected from the group consisting of water-soluble binders, mucilaginous excipients, water-dissolution aids, and mixtures thereof.

8. The composition of claim 7, wherein the additives are selected from the group consisting of methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxypropyl methylcellulose, polyacrylic acids, fats, and mixtures thereof.

9. The composition of claim 1 which comprises coated tablet cores prepared by compressing granules consisting of mopidamol or an acid addition salt thereof, acid or acid substance, lubricant, and other conventional additives to form tablet cores and then coating said tablet cores with a flavor-masking coating.

10. The composition of claim 1 which comprises coated cores prepared by (a) moist or dry granulation of (i) mopidamol 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 cores; and

(d) coating of said cores with a flavor-masking coating.

11. The composition of claim 1 which comprises coated cores prepared by (a) moist or dry granulation of (i) mopidamol or an acid addition salt thereof and (ii) conventional excipients to form a granulate;

(b) addition of acid or acid substance and lubricant to said granulate;

(c) compression of said granulate to form cores; and

(d) coating of said cores with a flavor-masking coating.

12. A method for the treatment of cardiovascular disorders or thrombosis in a host in need of such treatment which comprises administering to said host a cardiovascularly or antithrombotically effective amount of a composition of claim 1.