Formulations of Ramipril

• US 20070254030A1
• Filed: 07/13/2007
• Published: 11/01/2007
• Est. Priority Date: 03/24/2004
• Status: Active Grant

• Current Assignee: Reynir Eyjolfsson
• Original Assignee: Reynir Eyjolfsson
• Inventors: EYJOLFSSON, Reynir
• Granted Patent: US 7,589,064 B2
• Time in Patent Office: Days
• US Class Current: 424/464
• 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 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/407 condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
• CPC Class Codes: A61K 31/549 having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

Abstract

The present invention relates to stable tablet formulations of ramipril, optionally in combination with a diuretic.

Claims

1. A tablet formulation comprising:

a) 0.5-5.0% w/w of ramipril;

b) 50-95% w/w of calcium sulphate dihydrate; and

c) 0.1-5.0% w/w of sodium hydrogen carbonate,

optionally in combination with a disintegrant, binder and lubricant and other excipients.

2. The tablet formulation of claim 1, wherein the calcium sulphate dihydrate is Compactrol.

3. The tablet formulation of claim 1, further comprising a diuretic.

4. The tablet formulation of claim 3, wherein the diuretic is hydrochlorothiazide.

5. The tablet formulation of claim 3, wherein the diuretic is piretanide.

6. The tablet formulation of claim 1, wherein the disintegrant is pregelatinised starch.

7. The tablet formulation of claim 1, wherein the binder is pregelatinised starch.

8. The tablet formulation of claim 1, wherein the lubricant is sodium stearyl fumarate.

9. The tablet formulation of claim 1 containing

(a) 1.25 mg ramipril, wherein the amount of ramipril is 0.5-1.5% w/w,

(b) 85-90% w/w Compactrol,

(c) 0.5-1.5% w/w sodium hydrogen carbonate,

(d) 7-13% w/w starch pregelatinised, and

(e) 0.5-1.5% w/w sodium stearyl fumarate.

10. The tablet formulation of claim 1 containing

(a) 2.5 mg, 5 mg or 10 mg ramipril, wherein the amount of ramipril is 1.4-2.5% w/w,

(b) 78-95% w/w Compactrol,

(c) 1.4-2.5% w/w sodium hydrogen carbonate,

(d) 7-13% w/w starch pregelatinised, and

(e) 0.5-1.5% w/w sodium stearyl fumarate.

11. The tablet formulation of claim 1, containing

(a) 2.5 mg ramipril/12.5 mg hydrochlorothiazide or 5 mg ramipril/25 mg hydrochlorothiazide, wherein the amount of ramipril is 1.4-2.5% w/w,

(b) 8.5-10.5% w/w hydrochlorothiazide,

(c) 65-75% w/w Compactrol,

(d) 1.0-2.5% w/w sodium hydrogen carbonate,

(e) 12-18% w/w starch pregelatinised, and

(f) 0.5-1.5% w/w sodium stearyl fumarate.

12. The tablet formulation claim 1, containing

(a) 5 mg ramipril and 6 mg piretanide, wherein the amount of ramipril is 1.5-2.5% w/w and the amount of piretanide is 1.8-3.0% w/w,

(b) 65-85% w/w Compactrol,

(c) 3.0-5.0% w/w sodium hydrogen carbonate,

(d) 10-20% w/w starch pregelatinised, and

(e) 0.5-1.5% w/w sodium stearyl fumarate.