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Claims for Patent: 8,580,298

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Claims for Patent: 8,580,298

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): Najaraian; Thomas (Los Osos, CA), Tam; Peter Y. (Redwood City, CA), Wilson; Leland F. (Menlo Park, CA)
Assignee: Vivus, Inc. (Mountain View, CA)
Application Number:12/481,540
Patent Claims: 1. A unit dosage form for weight loss for oral administration to a patient having a body mass index of at least 30 kg/m.sup.2 and a condition associated with obesity, comprising a combination of: an immediate release phentermine formulation containing a unit dosage of phentermine in the range of 2 mg to 8 mg; and a controlled release topiramate formulation containing a unit dosage of topiramate in the range of 15 mg to 50 mg, wherein the dosage of phentermine in mg/day is about 16% of the dosage of topiramate in mg/day, and wherein the controlled release topiramate formulation reaches a maximum plasma concentration (Cmax) at about 6 to about 10 hours (Tmax) after administration and exhibits a lower Cmax, than non-controlled release topiramate, without decreasing total drug exposure defined by the area under the concentration-time curve (AUC), thereby enabling reduction of concentration-dependent side effects without a decrease in efficacy.

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

3. The dosage form of claim 2, comprising a capsule housing the immediate release phentermine beads and the controlled release topiramate beads.

4. 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.

5. The dosage form of claim 4, wherein the time period is in the range of about 6 to about 10 hours.

6. 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.

7. The dosage form of claim 1, wherein the controlled release topiramate formulation comprises controlled release beads of the topiramate, a binder, and a polymeric filler in a matrix core, wherein the matrix core is provided with a delayed release coating comprising ethyl cellulose and polyvinyl pyrrolidone.

8. The dosage form of claim 7, wherein the polymeric filler comprises microcrystalline cellulose.

9. The dosage form of claim 7, wherein the binder comprises methylcellulose.

10. The dosage form of claim 1, wherein the unit dosage of phentermine is in the range of 2 mg to 5 mg.

11. The dosage form of claim 1, wherein the unit dosage of topiramate is in the range of 15 mg to 25 mg.

12. The dosage form of claim 11, wherein the unit dosage of topiramate is in the range of 17 mg to 23 mg.

13. The dosage form of claim 10, wherein the unit dosage of topiramate is in the range of 15 mg to 25 mg.

14. The dosage form of claim 13, wherein the unit dosage of topiramate is in the range of 17 mg to 23 mg.

15. 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.

16. The dosage form of claim 15, wherein the 3.75 mg phentermine is in the form of 4.92 mg phentermine hydrochloride.

17. 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.

18. The dosage form of claim 17, wherein the 7.5 mg phentermine is in the form of 9.84 mg phentermine hydrochloride.

19. The dosage form of claim 7, wherein the ethyl cellulose and the polyvinyl pyrrolidone in the delayed release coating are in a weight ratio of approximately 2.3:1.

20. 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.

21. A unit dosage form for weight loss for oral administration to a patient having a body mass index of at least 30 kg/m.sup.2 and a condition associated with obesity, comprising a combination of: an immediate release phentermine formulation containing a unit dosage of phentermine in the range of 2 mg to 8 mg; and a controlled release topiramate formulation containing a unit dosage of topiramate in the range of 15 mg to 50 mg, comprising controlled release beads of the topiramate, a binder, and a polymeric filler in a matrix core, wherein the matrix core is provided with a delayed release coating comprising ethyl cellulose and polyvinyl pyrrolidone, and wherein the dosage of phentermine in mg/day is about 16% of the dosage of topiramate in mg/day, and wherein the controlled release topiramate formulation exhibits a maximum plasma concentration (Cmax) at about 6 to about 10 hours (Tmax) after administration and exhibits a lower Cmax, than non-controlled release topiramate, without decreasing total drug exposure defined by the area under the concentration-time curve (AUC), thereby enabling reduction of concentration-dependent side effects without a decrease in efficacy.

22. 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.

23. 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.

24. A packaged pharmaceutical preparation comprising a plurality of the unit dosage forms of claim 21 in a sealed container and instructions for administering the dosage forms orally to effect weight loss.

25. A packaged pharmaceutical preparation, comprising a plurality of the unit dosage forms of claim 21 each in a discrete sealed housing, and instructions for administering the dosage forms orally to effect weight loss.

26. The dosage form of claim 1 or 21, wherein the condition associated with obesity is selected 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.
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