Escalating dosing regimen for effecting weight loss and treating obesity
Inventors
Najarian, Thomas • Tam, Peter Y. • Wilson, Leland F.
Assignees
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Publication Number
US-8895057-B2
Publication Date
2014-11-25
Expiration Date
Abstract
The present invention is drawn to novel topiramate compositions as well as methods for effecting weight loss, e.g., in the treatment of obesity and related conditions, including conditions associated with and/or caused by obesity per se. The present invention features an escalating dosing regimen adapted for the administration of topiramate and optionally a sympathomimetic agent such as phentermine or bupropion, in the treatment of obesity and related conditions.
Core Innovation
The invention relates to a method for effecting weight loss in a patient having a body mass index of at least 25 kg/m2 by administering an escalating unit dosage form that includes controlled release topiramate and immediate release phentermine. The method uses a first dosage form administered daily for at least 2 weeks and a second dosage form administered daily for at least 2 years.
The escalating unit dosage form specifies controlled-release topiramate reaching maximum plasma concentration (Cmax) at about 6 to about 10 hours (Tmax) after administration, while exhibiting a lower Cmax than non-controlled release topiramate without decreasing total drug exposure defined by the area under the concentration-time curve (AUC). Immediate-release phentermine is part of the first and second dosage forms.
Representative controlled-release topiramate beads and immediate-release phentermine beads are described as suitable formulation forms within the dosage regimen. The summary further indicates a pharmacokinetic comparison showing reduced phentermine exposure characteristics for the controlled-release topiramate combination versus reference immediate-release topiramate.
Claims Coverage
The partial content includes two independent claims directed to weight loss treatment using an escalating unit dosage form comprising controlled-release topiramate and immediate-release phentermine, with specified dosing periods and pharmacokinetic behavior for controlled-release topiramate.
Escalating unit dosage form for weight loss with controlled-release topiramate and immediate-release phentermine
A method for effecting weight loss in a patient having a body mass index of at least 25 kg/m2, comprising administering an escalating unit dosage form comprising a first dosage form with 23 mg of topiramate formulated for controlled release and 3.75 mg of phentermine formulated for immediate release, wherein the first dosage form is administered to the subject daily for at least 2 weeks; and a second dosage form with 46 mg of topiramate formulated for controlled release and 7.5 mg of phentermine formulated for immediate release, wherein the topiramate formulated for controlled release reaches 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), and wherein the second dosage form is administered to the subject daily for at least 2 years, thereby effecting weight loss.
Escalating unit dosage form with higher controlled-release topiramate dose and extended dosing period
A method for effecting weight loss in a patient having a body mass index of at least 25 kg/m2, comprising administering an escalating unit dosage form comprising a first dosage form with 23 mg of topiramate formulated for controlled release and 3.75 mg of phentermine formulated for immediate release, wherein the first dosage form is administered to the subject daily for at least 2 weeks; and a second dosage form with 92 mg of topiramate formulated for controlled release and 15 mg of phentermine formulated for immediate release, wherein the topiramate formulated for controlled release reaches 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), and wherein the second dosage form is administered to the subject daily for at least 2 years, thereby effecting weight loss.
Across the independent claims, the core claimed coverage is an escalating dosing regimen using a unit dosage form that combines controlled-release topiramate and immediate-release phentermine, with a short initial daily period followed by a long daily maintenance period, and with controlled-release topiramate characterized by delayed Tmax and lower Cmax without decreased AUC.
Stated Advantages
Controlled-release topiramate exhibits a lower Cmax than non-controlled release topiramate without decreasing total drug exposure defined by AUC.
Controlled-release topiramate reaches maximum plasma concentration (Cmax) at about 6 to about 10 hours (Tmax) after administration.
The described pharmacokinetic comparison indicates reduced phentermine exposure characteristics for the controlled-release topiramate combination versus reference immediate-release topiramate.
Documented Applications
Treating weight loss in patients having a body mass index of at least 25 kg/m2 using an escalating unit dosage form.
The dependent claim set includes obesity-associated treatment indication selection based on an explicit list of medical conditions that includes diabetes-related conditions, cardiovascular conditions, respiratory conditions, and cancer among others.
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