Pharmaceutically acceptable salts

• US 4,879,303 A
• Filed: 10/13/1988
• Issued: 11/07/1989
• Est. Priority Date: 04/04/1986
• Status: Expired due to Term

• Current Assignee: Pfizer Inc.
• Original Assignee: Pfizer Inc.
• Inventors: Davison, Edward, Wells, James I.
• Primary Examiner(s): Fan, Jane T.
• Application Number:
  US07/256,938
• Time in Patent Office: 390 Days
• Field of Search: 514/356, 546/321
• US Class Current: 514/356
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/08 Vasodilators for multiple indications
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 Antihypertensives
• CPC Class Codes: C07D 211/90 Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Abstract

Improved pharmaceutical salts of amlodipine, particularly the besylate salt, and pharmaceutical compositions thereof. These salts find utility as anti-ischaemic and anti-hypertensive agents.

Claims

1. The besylate salt of amlodipine.

2. A pharmaceutical composition comprising an antihypertensive, antiischaemic or angina - alleviating effective amount of the besylate salt of amlodipine as claimed in claim 1 together with a pharmaceutically acceptable diluent or carrier.

3. A tablet formulation comprising an anti-hypertensive, antiischaemic or angina - alleviating effective amount of the besylate salt of amlodipine as claimed in claim 1 in admixture with excipients.

4. A tablet formulation as claimed in claim 3 wherein the excipients comprise a compression and, an additive to provide sheen to the tablet, a disintegrant and a lubricant.

5. A tablet formulation as claimed in claim 4 wherein the excipients comprise microcrystalline cellulose, anhydrous dibasic calcium phosphate, sodium starch glycollate and magnesium stearate.

6. A capsule formulation comprising an antihypertensive, antiischaemic or angina - alleviating effective amount of the besylate salt of amlodipine as claimed in claim 1 in admixture with excipients.

7. A capsule formulation as claimed in claim 6 wherein the excipients comprise an inert diluent, a dried disintegrant and a lubricant.

8. A capsule formulation as claimed in claim 7 wherein the excipients comprise microcrystalline cellulose, dried maize starch and magnesium stearate.

9. A sterile aqueous solution comprising an antihypertensive, antiischaemic or angina - alleviating effective amount of the besylate salt of amlodipine for parenteral administration.

10. A sterile aqueous solution as claimed in claim 9 comprising from 10 to 40% w/v of propylene glycol.

11. A sterile aqueous solution as claimed in claim 9 or claim 10 comprising about 1% w/v sodium chloride.