A new method for the preparation of pure topiramate with a micron particle size

Abstract

Crude topiramate was prepared from the reaction between diacetonefructopyranose, sulfuric diamide, and 2-picoline. During a controlled processing the presence of Triton-X-100, crude topiramate in a methanol-water solvent, was converted to pure micron size topiramate particles. The factors affecting the purification and micronization of topiramate, such as solvent and anti-solvent type and concentration ratio, temperature, and mixing speed, were investigated. A mechanism for the preparation of topiramate was proposed based on the results of changes in the concentration of the raw materials and an investigation of the intermediates. In addition, the solubility rate of topiramate with different particle sizes has been determined.

Keywords

• Topiramate
• Particle size
• Micronized drugs
• Solubility