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

• Main Authors: KÄLZ, BEATE, GAETA, FEDERICO, ROTHENBURGER, JAN, GERDES, KLAUS, WELZIG, STEFAN, GUNGL, JÓZSEF
• Format: Patent
• Language: English; French; German
• Published: 01.06.2016
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

2,4'-Dimethyl-3-piperidino propiophenone (tolperisone) and their pharmaceutical acceptable salts production involves converting 4-methylpropiophenone with piperidinhydrochloride and 1,2-dioxolane in presence of one or multiple acids as catalyst in a solvent. The tolperisone raw product is filtered in the form of pharmaceutical compatible hydrochlorides, hydrates, and addition salts after cooling the reaction mixture. A part is reduced to 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) by recrystallization of the tolperisone raw product in presence of a counter solvent and absorbent. Independent claims are included for: (1) a method for producing a pharmaceutical formulation, which involves blending tolperisone as active substance under water-free conditions in one or multiple solvents with a water-free additive in the form of a pharmaceutical compatible acid, preferably citric acid; (2) a controlled release (CR) formulation, which comprises a core component and a retard coating; and (3) a transdermal therapeutic system, which comprises a reservoir layer containing tolperisone as active substance in pure form. ACTIVITY : Neuroprotective; Nootropic. MECHANISM OF ACTION : None given.