Low dose topiramate/phentermine composition and methods of use thereof

Inventors

Najarian, Thomas • Tam, Peter Y. • Wilson, Leland F.

Assignees

Vivus LLC

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.

Core Innovation

The described invention relates to a unit dosage form for weight loss for oral administration to a patient having a body mass index of at least 25 kg/m2. The unit dosage form comprises a combination of an immediate release phentermine formulation and a controlled release topiramate formulation. The immediate release phentermine formulation provides a unit dosage of phentermine of 3.75 mg or 7.5 mg, and the controlled release topiramate formulation provides a unit dosage of topiramate of 23 mg or 46 mg.

A defining feature is that the controlled release topiramate formulation reaches a maximum plasma concentration (Cmax) at about 6 to about 10 hours (Tmax) after administration. The described formulations include controlled release topiramate beads and immediate release phentermine beads. The disclosure further includes pharmacokinetic comparisons using parameters such as AUC, Cmax, Tmax, and t1/2.

The patent text further describes exemplary dosing regimens and administration schedules in which the immediate-release phentermine is administered together with a lower daily dose of topiramate selected to maintain phentermine efficacy and reduce side effects. The described controlled/sustained/delayed release topiramate concept includes a delayed Tmax in a window of about 6 to about 10 hours. The disclosure also provides formulation composition concepts using controlled release topiramate beads and immediate release phentermine beads, along with examples showing pharmacokinetic and patient-case outcomes.

Claims Coverage

The partial content provides one independent claim. The independent claim covers an oral unit dosage form for weight loss that combines specific unit doses of immediate-release phentermine and controlled-release topiramate, with a defined Tmax window for topiramate Cmax (about 6 to about 10 hours).

Overall, the claim coverage centers on combining a specified immediate-release phentermine unit dose with a specified controlled-release topiramate unit dose for oral weight loss in patients with BMI at least 25 kg/m2, while achieving a controlled-release topiramate Tmax window of about 6 to about 10 hours after administration.

Stated Advantages

Documented Applications

No documented applications found