composições de tolperisona

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 filte...

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Bibliographic Details
Main Authors Jan Rothenburger, Stefan Welzig, Klaus Gerdes, Frederico Gaeta, Beate Kälz, József Gungl
Format Patent
LanguagePortuguese
Published 09.05.2017
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary: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.
Bibliography:Application Number: BR2008PI10670