Pharmaceutical composition containing proton pump inhibitors

• US 6,316,481 B1
• Filed: 02/22/2000
• Issued: 11/13/2001
• Est. Priority Date: 02/23/1999
• Status: Expired due to Term

• Current Assignee: Merck Sharp & Dohme Corporation (Merck & Co., Inc.)
• Original Assignee: Merck & Co., Inc.
• Inventors: Freehauf, Keith
• Primary Examiner(s): Weddington, Kevin E.
• Application Number:
  US09/510,312
• Time in Patent Office: 630 Days
• Field of Search: 514/393, 514/394
• US Class Current: 514/393
• CPC Class Codes: A61K 31/4439 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole nicotine A61K31/465
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

Abstract

The present invention is concerned with an oral pharmaceutical formulation containing a proton pump inhibitor (PPI) which is suitable for the treatment of gastric acid related diseases in man and animals. More specifically, the composition is a paste, and is particularly suitable for delivery of a proton pump inhibitor to horses.

Claims

1. A pharmaceutical formulation for oral administration comprising:

(a) about 1% to about 60% w/w of omeprazole,

(b) about 0.1% to about 2% w/w of two to four basifying agents,

(c) about 1% to about 3% w/w of a thickening agent, and

(d) a hydrophobic oily liquid vehicle comprising

(i) a vegetable oil and

(ii) triglycerides of medium chain fatty acids or propylene glycol diesters of medium chain fatty acids.

2. A composition of claim 1 wherein said thickening agent is hydrogenated castor oil.

3. A composition of claim 1 wherein said hydrophobic liquid vehicle comprises propylene glycol caprate/caprylate and a vegetable oil.

4. A composition of claim 1 wherein said hydrophobic liquid vehicle comprises sesame oil and triglycerides of medium chain fatty acids or propylene glycol diesters of medium chain fatty acids.

5. A composition of claim 1 wherein said hydrophobic liquid vehicle comprises propylene glycol caprate/caprylate and sesame oil.

6. A composition of claim 1 wherein one of the basifying agents is potassium sorbate.

7. A composition of claim 1 wherein the basifying agents are potassium sorbate, sodium stearate and monoethanolamine.

8. A composition of claim 1 wherein the amount of omeprazole is about 30 to about 40% w/w.

9. A composition of claim 1 wherein the total amount of basifying agents is from about 1 to about 1.5% w/w.

10. A composition of claim 1 wherein the amount of the hydrophobic oily liquid vehicle is about 30% to 90% w/w.

11. A composition of claim 1 wherein the amount of the hydrophobic oily liquid vehicle is about 50% to 80% w/w.