Pharmaceutical composition of aspirin and a benzothiazepine for inhibiting platelet aggregation

• US 5,387,581 A
• Filed: 03/23/1993
• Issued: 02/07/1995
• Est. Priority Date: 09/17/1990
• Status: Expired due to Fees

• Current Assignee: Tanabe Seiyaku Co Ltd (Mitsubishi Chemical Group Corp.)
• Original Assignee: Tanabe Seiyaku Co Ltd (Mitsubishi Chemical Group Corp.)
• Inventors: Sasaki, Yasuhiko, Narita, Hiroshi, Murata, Sakae, Odawara, Akio
• Primary Examiner(s): Cintins, Marianne M.
• Assistant Examiner(s): CRIARES, THEODORE J
• Application Number:
  US08/035,895
• Time in Patent Office: 686 Days
• Field of Search: 514/211, 514/165
• US Class Current: 514/165
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 31/60 Salicylic acid; Derivatives thereof

Abstract

There is disclosed a pharmaceutical composition for inhibiting the platelet aggregation comprising acetylsalicyclic acid or a pharmaceutically acceptable salt thereof and a 1,5-benzothiazepine derivative of the formula: ##STR1## wherein R¹ is a lower alkyl group or a lower alkoxy group, R² is hydrogen atom or a lower alkanoyl group, R³ is a lower alkyl group, R⁴ is hydrogen atom or a lower alkyl group and R⁵ is a lower alkyl group or a halogen atom, or a pharmaceutically acceptable salt thereof.

Claims

1. A pharmaceutical composition for inhibiting platelet aggregation, which comprises acetylsalicylic acid and (-)-cis-2-(4-methylphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one maleate, wherein the weight ratio of acetylsalicylic acid to (-)-cis-2-(4-methylphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one maleate is 0.3-40:

1.

2. The composition according to claim 1, wherein the weight ratio of acetylsalicylic acid to (-)-cis-2-(4-methylphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one maleate is 1-10:

1.

3. The composition according to claim 1, wherein acetylsalicylic acid is present in an amount to provide a dosage level of 20 to 200 mg per day and (-)-cis-2-(4-methylphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one maleate is present in an amount to provide a dosage level of 5 to 60 mg per day.

4. The composition according to claim 1, wherein acetylsalicylic acid is present in an amount to provide a dosage level of 30 to 100 mg per day and (-)-cis-2-(4-methylphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one maleate is present in an amount to provide a dosage level of 10 to 30 mg per day.

5. The composition according to claim 2, wherein acetylsalicylic acid is present in an amount to provide a dosage level of 20 to 200 mg per day and (-)-cis-2-(4-methylphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one maleate is present in an amount to provide a dosage level of 5 to 60 mg per day.

6. The composition according to claim 2, wherein acetylsalicylic acid is present in an amount to provide a dosage level of 30 to 100 mg per day and (-)-cis-2-(4-methylphenyl)-3-acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one maleate is present in an amount to provide a dosage level of 10 to 30 mg per day.