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Claims for Patent: 9,011,905

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Claims for Patent: 9,011,905

Title:Low dose topiramate/phentermine composition and methods of use thereof
Abstract: A method for effecting weight loss by administering a combination of topiramate and phentermine is provided. The phentermine is generally administered in immediate release form, in a daily dose in the range of 2 mg to 8 mg, in combination with a daily dose of topiramate selected to prevent the loss of effectiveness of phentermine alone. Methods for treating obesity, conditions associated with obesity, and other indications are also provided, as are compositions and dosage forms containing low doses of phentermine and topiramate, e.g., 3.75 mg phentermine and 23 mg topiramate.
Inventor(s): Najarian; Thomas (Los Osos, CA), Tam; Peter Y. (Redwood City, CA), Wilson; Leland F. (Menlo Park, CA)
Assignee: Vivus, Inc. (Mountain View, CA)
Application Number:14/495,246
Patent Claims: 1. A unit dosage form for weight loss for oral administration to a patient having a body mass index of at least 25 kg/m.sup.2, comprising a combination of: an immediate release phentermine formulation containing a unit dosage of phentermine of 3.75 mg or 7.5 mg; and a controlled release topiramate formulation containing a unit dosage of topiramate of 23 mg or 46 mg, wherein the controlled release topiramate formulation reaches a maximum plasma concentration (Cmax) at about 6 to about 10 hours (Tmax) after administration.

2. The dosage form of claim 1, wherein the subject is overweight having a body mass index between 25 kg/m.sup.2 and 29.9 kg/m.sup.2.

3. The dosage form of claim 2, wherein the subject has a condition associated with obesity.

4. The dosage form of claim 1, wherein the subject is obese having a body mass index of at least 30 kg/m.sup.2.

5. The dosage form of claim 4, wherein the condition associated with obesity is selected from the group consisting of diabetes, elevated fasting blood glucose, insulin resistance, impaired glucose tolerance, pulmonary hypertension, asthma, shortness of breath, gallbladder disease, dyslipidemia, high cholesterol, high levels of triglycerides, osteoarthritis, reflux esophagitis, sleep apnea, menstrual irregularities, infertility, complications in pregnancy, gout, high blood pressure, hypertension, coronary artery disease, heart disease, muscular dystrophy, stroke, thrombotic stroke, deep vein thrombosis (DVT), migraines, metabolic disorders, hypoalphalipoproteinemia, familial combined hyperlipidemia, Syndrome X, insulin-resistant Syndrome X, colon cancer, rectal cancer, renal cancer, esophageal cancer, gallbladder cancer, pancreatic cancer, prostate cancer, breast cancer, uterine cancer, ovarian cancer, endometrial cancer, and cervical cancer.

6. The dosage form of claim 3, wherein the condition associated with obesity is selected from the group consisting of hypertension, dyslipidemia, and type 2 diabetes mellitus.

7. The dosage form of claim 3, wherein the subject is suffering from at least two conditions associated with obesity selected from the group consisting of hypertension, dyslipidemia, and type 2 diabetes mellitus.

8. The dosage form of claim 1, wherein the topiramate formulated for controlled release further exhibits a lower Cmax, than non-controlled release topiramate, without decreasing total drug exposure defined by the area under the concentration-time curve (AUC).

9. The dosage form of claim 1, wherein the unit dosage of phentermine is 3.75 mg and the unit dosage of topiramate is 23 mg.

10. The dosage form of claim 9, wherein the 3.75 mg phentermine is provided in the unit dosage form as about 4.92 mg phentermine hydrochloride, and wherein 4.92 mg of phentermine hydrochloride provides 3.75 mg of phentermine.

11. The dosage form of claim 1, wherein the unit dosage of phentermine is 7.5 mg and the unit dosage of topiramate is 46 mg.

12. The dosage form of claim 11, wherein the 7.5 mg phentermine is provided in the unit dosage form as about 9.84 mg phentermine hydrochloride, and wherein 9.84 mg of phentermine hydrochloride provides 7.5 mg of phentermine.

13. The dosage form of claim 1, wherein following oral administration to a patient, the dosage form provides for a substantially constant blood level of topiramate over a time period in the range of about 4 to about 12 hours.

14. The dosage form of claim 13, wherein the time period is in the range of about 6 to about 10 hours.

15. The dosage form of claim 1, wherein the controlled release topiramate formulation reaches a maximum plasma concentration at about 8 hours to about 10 hours (Tmax) after administration.

16. The dosage form of claim 1, wherein the immediate release phentermine formulation comprises beads of inactive cores coated with the immediate release phentermine formulation.

17. The dosage form of claim 16, comprising a capsule housing the immediate release phentermine beads and the controlled release topiramate beads.

18. The dosage form of claim 1, wherein the controlled release topiramate formulation comprises beads comprising a core comprising topiramate dispersed in a gradually hydrolysable material comprising a binder, and a polymeric filler, and wherein the core is provided with a delayed release coating.

19. The dosage form of claim 18, wherein the delayed release coating comprises one or more of ethylcellulose, hydroxypropyl methylcellulose, microcrystalline cellulose, hydroxypropyl cellulose, polyvinyl acetate, ethylene-vinyl acetate copolymer and polyvinyl pyrrolidone.

20. The dosage form of claim 18, wherein the delayed release coating comprises ethylcellulose and polyvinyl pyrrolidone.

21. The dosage form of claim 18, wherein the polymeric filler comprises microcrystalline cellulose.

22. The dosage form of claim 21, wherein the microcrystalline cellulose has a particle size of 50 microns to 200 microns.

23. The dosage form of claim 18, wherein the binder comprises methylcellulose.

24. The dosage form of claim 20, wherein the ethyl cellulose and the polyvinyl pyrrolidone in the delayed release coating are in a weight ratio of approximately 2.3:1.

25. The dosage form of claim 1, comprising a tablet with at least two discrete segments, at least one of which contains the immediate release phentermine formulation and at least another of which contains the controlled release topiramate formulation.

26. The dosage form of claim 1, wherein the controlled release topiramate formulation comprises beads comprising topiramate dispersed within a delayed release matrix comprising methylcellulose, microcrystalline cellulose, ethylcellulose and polyvinyl pyrrolidine.

27. The dosage form of claim 1, wherein the controlled release topiramate formulation comprises beads comprising topiramate dispersed within a delayed release matrix comprising hydroxypropyl methyl cellulose.

28. The dosage form of claim 1, wherein the controlled release topiramate formulation comprises beads comprising topiramate dispersed within a delayed release matrix and comprising a polymer selected from methylcellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, cellulose acetate, methacrylic acid copolymer and ethylcellulose.

29. The dosage form of claim 1, wherein the controlled release topiramate formulation comprises a topiramate dosage form coated by a gradually hydrolysable material.

30. The dosage form of claim 29 wherein the gradually hydrolysable material comprises one or more of ethylcellulose, povidone, microcrystalline cellulose and hydroxypropyl methylcellulose.

31. The dosage form of claim 1, wherein the controlled release topiramate formulation comprises a core comprising topiramate, microcrystalline cellulose and methylcellulose and wherein the core is coated with ethyl cellulose and povidone.

32. The dosage form of claim 8, wherein the unit dosage of phentermine is 3.75 mg and the unit dosage of topiramate is 23 mg.

33. The dosage form of claim 8, wherein the unit dosage of phentermine is 7.5 mg and the unit dosage of topiramate is 46 mg.

34. The dosage form of claim 8, wherein the controlled release topiramate formulation reaches a maximum plasma concentration at about 8 hours to about 10 hours (Tmax) after administration.

35. The dosage form of claim 8, wherein the controlled release topiramate formulation comprises beads comprising a core comprising topiramate dispersed in a gradually hydrolysable material comprising a binder, and a polymeric filler, and wherein the core is provided with a delayed release coating.

36. The dosage form of claim 8, wherein the controlled release topiramate formulation comprises a core comprising topiramate, microcrystalline cellulose and methylcellulose and wherein the core is coated with ethyl cellulose and povidone.

37. A packaged pharmaceutical preparation comprising a plurality of the unit dosage forms of claim 1 in a sealed container and instructions for administering the dosage forms orally to effect weight loss.

38. A packaged pharmaceutical preparation, comprising a plurality of the unit dosage forms of claim 1 each in a discrete sealed housing, and instructions for administering the dosage forms orally to effect weight loss.
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