Title:
CRYSTALLINE TOLTERODINE TARTARATE AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
Document Type and Number:
WIPO Patent Application WO2008017278
Kind Code:
B1
Abstract:
A crystalline salt of 2-[(1R)-3-[bis(l-methylethyl)amino]-1-?henyl?ropyl]-4-methyl-phenol with (2R,3R)-2,3-dihydroxybutanedioic acid, known under the name R-tolterodine tartarate, wherein: a) at least 90 % of all crystals are present in a size smaller than 30 µm, b) at least 40 % of crystalline matter are smaller than 250 µm, c) the maximum size of crystals does not exceed 800 µm, d) the salt contains less than 0.1 weight % of the undesirable enantiomer S-tolterodine tartarate, e) analytical test for sulfate ashes (Pharm. Eur.) provides a value lower than 0.1%. The method of its preparation involves at least one crystallization from water. A pharmaceutical composition containing tolterodine or its pharmaceutically acceptable salts further contains a filler, a disintegrant and a lubricant, said composition being free of ions of alkaline earth metals.
Inventors:
SVOBODA MARTIN (CZ)
JAMPILEK JOSEF (CZ)
KACIRKOVA MARTINA (CZ)
TOMASEK VACLAV (CZ)
LEHOCKY MIKULAS (CZ)
HEJTMANKOVA LUDMILA (CZ)
VOSATKA VACLAV (CZ)
JAMPILEK JOSEF (CZ)
KACIRKOVA MARTINA (CZ)
TOMASEK VACLAV (CZ)
LEHOCKY MIKULAS (CZ)
HEJTMANKOVA LUDMILA (CZ)
VOSATKA VACLAV (CZ)
Application Number:
PCT/CZ2007/000078
Publication Date:
August 28, 2008
Filing Date:
August 09, 2007
Export Citation:
Assignee:
ZENTIVA AS (CZ)
SVOBODA MARTIN (CZ)
JAMPILEK JOSEF (CZ)
KACIRKOVA MARTINA (CZ)
TOMASEK VACLAV (CZ)
LEHOCKY MIKULAS (CZ)
HEJTMANKOVA LUDMILA (CZ)
VOSATKA VACLAV (CZ)
SVOBODA MARTIN (CZ)
JAMPILEK JOSEF (CZ)
KACIRKOVA MARTINA (CZ)
TOMASEK VACLAV (CZ)
LEHOCKY MIKULAS (CZ)
HEJTMANKOVA LUDMILA (CZ)
VOSATKA VACLAV (CZ)
International Classes:
C07C213/10; A61K31/137; C07C215/54
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