METHOD FOR THE PRODUCTION OF HIGHLY PURE 2,4'-DIMETHYL-3-PIPERIDINO-PROPIOPHENONE (TOLPERISONE), PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND AGENT FORMULATIONS CONTAINING TOLPERISONE

摘要

The invention relates to a method for producing highly pure 2,4'-dimethyl-3-piperidino-propiophenone (tolperisone) and the pharmaceutically acceptable salts, hydrochlorides, and hydrates thereof. Said method allows the content of the undesired byproduct 2-methyl-1-(4-methyphenyl) 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.