Invention Application
WO2008017278A2 CRYSTALLINE TOLTERODINE TARTARATE AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
审中-公开
结晶酒石酸酒石酸盐和含有相同物质的药物组合物
- Patent Title: CRYSTALLINE TOLTERODINE TARTARATE AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
- Patent Title (中): 结晶酒石酸酒石酸盐和含有相同物质的药物组合物
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Application No.: PCT/CZ2007/000078Application Date: 2007-08-09
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Publication No.: WO2008017278A2Publication Date: 2008-02-14
- Inventor: SVOBODA, Martin , JAMPILEK, Josef , KACIRKOVA, Martina , TOMASEK, Vaclav , LEHOCKY, Mikulas , HEJTMANKOVA, Ludmila , VOSATKA, Vaclav
- Applicant: ZENTIVA, A.S. , SVOBODA, Martin , JAMPILEK, Josef , KACIRKOVA, Martina , TOMASEK, Vaclav , LEHOCKY, Mikulas , HEJTMANKOVA, Ludmila , VOSATKA, Vaclav
- Applicant Address: U kabelovny 130 102 37 Praha 10 CZ
- Assignee: ZENTIVA, A.S.,SVOBODA, Martin,JAMPILEK, Josef,KACIRKOVA, Martina,TOMASEK, Vaclav,LEHOCKY, Mikulas,HEJTMANKOVA, Ludmila,VOSATKA, Vaclav
- Current Assignee: ZENTIVA, A.S.,SVOBODA, Martin,JAMPILEK, Josef,KACIRKOVA, Martina,TOMASEK, Vaclav,LEHOCKY, Mikulas,HEJTMANKOVA, Ludmila,VOSATKA, Vaclav
- Current Assignee Address: U kabelovny 130 102 37 Praha 10 CZ
- Agency: JIROTKOVA, Ivana et al.
- Priority: CZPV 20060809; CZPV 20070226
- Main IPC: C07C213/10
- IPC: C07C213/10 ; C07C215/54 ; A61K31/137
Abstract:
A crystalline salt of 2-[(1R)-3-[bis(l-methylethyl)amino]-1-ρhenylρropyl]-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.
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