Process for the production of high-purity 2,4′-dimethyl-3-piperidino-propiophenone (tolperisone), pharmaceutical compositions that contain the latter, as well as active ingredient formulations that contain tolperisone

US8372979B2 · kind B2 · utility

Assignee

• SANOCHEMIA PHARMAZEUTIKA AG · AU

Inventors

• Stefan Welzig · Wien, AT
• Jan Rothenburger · Eisenstadt, AT
• Beate Kalz · Steinbrunn, AT
• Jozsef Gungl · Ágfalva, HU
• Klaus Gerdes · Düsseldorf, DE
• Federico Gaeta · Carrión de los Condes, ES

Key dates

• Filing date: Apr 24, 2008
• Grant date: Feb 12, 2013
• Expiry date: May 6, 2029

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10T436/145555
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to a method for producing highly pure 2,4′-dimethyl-3-piperidino-propiophenone (tolperisone) (formula I) and the pharmaceutically acceptable salts, hydrochlorides, and hydrates thereof. The method allows the content of the undesired byproduct 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) to be kept significantly lower than in previously known methods. The invention further relates to active substance formulations which contain tolperisone and are suitable, among other things, for producing combination preparations used for treating patients suffering from Alzheimer's disease. The invention also relates to topical formulations, controlled release (CR) formulations, and transdermal therapeutic systems, such as active substance patches, which contain less than 50 ppm, preferably less than 10 ppm, more preferably less than 7 ppm, and most preferably less than 3 ppm or 0 ppm (i.e. less than the detectable amount) of the undesired byproduct 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) in relation to 100 percent by weight of active substance.