Claims for Patent: 9,364,439

Summary for Patent: 9,364,439

Title:	Pharmaceutical compositions for the coordinated delivery of NSAIDs
Abstract:	The present invention is directed to drug dosage forms that release an agent that raises the pH of a patient's gastrointestinal tract, followed by a non-steroidal anti-inflammatory drug. The dosage form is designed so that the NSAID is not released until the intragastric pH has been raised to a safe level. The invention also encompasses methods of treating patients by administering this coordinated release, gastroprotective, antiarthritic/analgesic combination unit dosage form to achieve pain and symptom relief with a reduced risk of developing gastrointestinal damage such as ulcers, erosions and hemorrhages.
Inventor(s):	Plachetka; John R. (Chapel Hill, NC)
Assignee:	Pozen Inc. (Chapel Hill, NC)
Application Number:	14/956,645
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,364,439
Patent Claims:	1. A pharmaceutical composition in unit dosage form suitable for oral administration to a patient, comprising therapeutically effective amounts of: (a) omeprazole, wherein at least a portion of the omeprazole is not surrounded by an enteric coating; and (b) aspirin surrounded by a coating that inhibits its release from the unit dosage form unless the unit dosage form is in a medium with a pH of 3.5 or higher; wherein the unit dosage form provides for release of omeprazole such that upon introduction of the unit dosage form into a medium, at least a portion of the omeprazole is released regardless of the pH of the medium. 2. The pharmaceutical composition of claim 1, wherein aspirin is present in the unit dosage form in an amount of from 40 to 100 mg. 3. The pharmaceutical composition of claim 1, wherein aspirin is present in the unit dosage form in an amount of from 250 to 1000 mg. 4. The pharmaceutical composition of claim 1, wherein aspirin is present in the unit dosage form in an amount of from 40 to 100 mg and omeprazole is present in the unit dosage form in an amount of from 5 to 50 mg. 5. The pharmaceutical composition of claim 1, wherein aspirin is present in the unit dosage form in an amount of from 250 to 1000 mg and omeprazole is present in the unit dosage form in an amount of from 5 to 50 mg. 6. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition further comprises one or more excipients selected from the group consisting of starch, polyethylene glycol, microcrystalline cellulose and hydroxymethylcellulose. 7. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition further comprises one or more materials selected from the group consisting of methacrylic acid copolymers, triethyl citrate, triacetin, polyethylene glycol, titanium dioxide and polysorbate. 8. The pharmaceutical composition of claim 1, wherein the coating surrounding the core does not dissolve unless the pH of the surrounding medium is at least 4. 9. The pharmaceutical composition of claim 1, wherein the coating surrounding the core does not dissolve unless the pH of the surrounding medium is at least 5. 10. The pharmaceutical composition of claim 1, wherein the unit dosage form is a bilayer tablet. 11. The pharmaceutical composition of claim 1, wherein the unit dosage form is a multilayer tablet. 12. The pharmaceutical composition of claim 4, wherein the unit dosage form is formulated for once daily administration. 13. The pharmaceutical composition of claim 5, wherein the unit dosage form is formulated for once daily administration. 14. A method of reducing the risk of stroke or heart attack in a patient, comprising administering to the patient a therapeutically effective amount of the pharmaceutical composition of claim 1. 15. The method of claim 14, wherein the pharmaceutical composition is administered to reduce the risk of stroke. 16. The method of claim 14, wherein the pharmaceutical composition is administered to reduce the risk of heart attack. 17. A method of reducing the incidence of NSAID-associated gastric ulcers in a patient who is at risk of developing such ulcers, wherein the method comprises administering to the patient in need thereof a pharmaceutical composition in unit dosage form comprising therapeutically effective amounts of: (a) omeprazole, wherein at least a portion of the omeprazole is not surrounded by an enteric coating; and (b) aspirin surrounded by a coating that inhibits its release from the unit dosage form unless the unit dosage form is in a medium with a pH of 3.5 or higher; wherein the unit dosage form provides for release of omeprazole such that upon introduction of the unit dosage form into a medium, at least a portion of the omeprazole is released regardless of the pH of the medium, wherein the pharmaceutical composition in unit dosage form reduces the incidence of NSAID-associated gastric ulcers in the patient. 18. The method of claim 17, wherein aspirin is present in the unit dosage form in an amount of from 40 to 100 mg and omeprazole is present in the unit dosage form in an amount of from 5 to 50 mg. 19. The method of claim 17, wherein aspirin is present in the unit dosage form in an amount of from 250 to 1000 mg and omeprazole is present in the unit dosage form in an amount of from 5 to 50 mg. 20. The pharmaceutical composition of claim 17, wherein the coating surrounding the core does not dissolve unless the pH of the surrounding medium is at least 4. 21. The method of claim 17, wherein the coating surrounding the core does not dissolve unless the pH of the surrounding medium is at least 5. 22. The method of claim 17 wherein the unit dosage form is a multilayer tablet. 23. The method of claim 17, wherein the unit dosage form is administered once daily. 24. A method of reducing the incidence of NSAID-associated gastric ulcers in a patient who is at risk of developing such ulcers, wherein the method comprises administering to the patient a pharmaceutical composition in unit dosage form comprising therapeutically effective amounts of: (a) omeprazole, or a pharmaceutically acceptable salt thereof, in a form and route sufficient to raise the gastric pH of the patient to at least 3.5 upon administration of one or more of the unit dosage forms; and (b) aspirin surrounded by a coating that inhibits its release from the unit dosage form unless the unit dosage form is in a medium with a pH of 3.5 or higher; wherein the unit dosage form provides for coordinated release of the omeprazole and the aspirin, wherein at least a portion of the omeprazole, or a pharmaceutically acceptable salt thereof, is released independent of the pH of the surrounding medium, wherein the pharmaceutical composition in unit dosage form reduces the incidence of NSAID-associated gastric ulcers in the patient. 25. The method of claim 24, wherein aspirin is present in the unit dosage form in an amount of from 40 to 100 mg and omeprazole is present in the unit dosage form in an amount of from 5 to 50 mg. 26. The method of claim 24, wherein aspirin is present in the unit dosage form in an amount of from 250 to 1000 mg and omeprazole is present in the unit dosage form in an amount of from 5 to 50 mg. 27. The pharmaceutical composition of claim 24, wherein the coating surrounding the core does not dissolve unless the pH of the surrounding medium is at least 4. 28. The method of claim 24, wherein the coating surrounding the core does not dissolve unless the pH of the surrounding medium is at least 5. 29. The method of claim 24, wherein the unit dosage form is a multilayer tablet. 30. The method of claim 24, wherein the unit dosage form is administered once daily.