Formulations of ramipril

• US 7,589,064 B2
• Filed: 07/13/2007
• Issued: 09/15/2009
• Est. Priority Date: 03/24/2004
• Status: Expired due to Fees

• Current Assignee: Actavis Group hf (Teva Pharmaceutical Industries Limited)
• Original Assignee: Actavis Group hf (Teva Pharmaceutical Industries Limited)
• Inventors: Eyjolfsson, Reynir
• Primary Examiner(s): Richter; Johann R
• Assistant Examiner(s): Soroush; Ali
• Application Number:
  US11/777,849
• Publication Number:
  US 20070254030A1
• Time in Patent Office: 795 Days
• Field of Search: 514/16
• US Class Current: 514/1.1
• 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) 1.25 mg ramipril, wherein the amount of ramipril is 0.5-1.5% w/w,

b) 85-90% w/w of calcium sulphate dihydrate,

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

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

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

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

3. The tablet formulation of claim 2, wherein the diuretic is hydrochiorothiazide.

4. The tablet formulation of claim 2, wherein the diuretic is piretanide.

11. The tablet formulation of claim 1, consisting essentially of:

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

b) 8 5-90% w/w of calcium sulphate dihydrate,

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

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

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

5. A tablet formulation comprising:

(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 calcium sulphate dihydrate,

(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.

8. The tablet formulation of claim 5, further comprising a diuretic.

9. The tablet formulation of claim 8, wherein the diuretic is hydrochlorothiazide.

10. The tablet formulation of claim 8, wherein the diuretic is piretanide.

12. The tablet formulation of claim 5, consisting essentially of:

(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 calcium sulphate dihydrate,

(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.

6. A tablet formulation comprising:

(a) 2.5 mg ramipril/12.5 mg hydrochiorothiazide 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 calcium sulphate dihydrate,

(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.

13. The tablet formulation of claim 6, consisting essentially of:

(a) 2.5 mg ramipril/12.5 mg hydrochlorothiazide or 5 mg ramipril/25 mg hydrochiorothiazide, 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 calcium sulphate dihydrate,

(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.

7. A tablet formulation comprising:

(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 calcium sulphate dihydrate,

(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.

14. The tablet formulation of claim 7, consisting essentially of:

(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 calcium sulphate dihydrate,

(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.