Stabilized pharmaceutical compositions comprising a calcium...

A - Human Necessities – 61 – K

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A61K 31/4427 (2006.01) A61K 9/20 (2006.01) A61K 9/48 (2006.01) A61K 47/02 (2006.01) A61P 9/12 (2006.01)

Patent

CA 2405046

The present invention provides a pharmaceutical composition containing a calcium blocker of the following formula or a pharmacologically acceptable salt thereof and a pharmacologically acceptable alkaline material which is added to an extent such that an aqueous solution or dispersion solution of said pharmaceutical composition containing a calcium blocker has a pH of at least 8: (see formula I) [wherein R1 represents an optionally substituted C1-C4 alkyl group, an amino group or a cyano group; R2 represents an optionally substituted C1-C4 alkyl group, a substituted C3-C4 alkenyl group, or a substituted 4- to 6-membered cyclic amino group; R3 represents a substituted phenyl group; R4 represents an optionally substituted C1-C4 alkoxycarbonyl group, a 1,3,2-phosphorinan-2-yl group, or a 5,5-dimethyl-1,3,2-phosphorinan-2-yl group, R5 represents a C1-C4 alkyl group].

Composition pharmaceutique contenant un bloqueur des canaux calcium et présentant une excellente stabilité à la conservation. Cette composition comprend un bloqueur des canaux calcium représenté par la formule (A) ou un de ses sels acceptable sur le plan pharmacologique et un milieu alcalin acceptable sur le plan pharmacologique et capable de conférer un pH égal ou supérieur à 8 à une solution aqueuse ou à une dispersion de cette composition : dans laquelle R<1> représente alkyle C1-C4 éventuellement substitué, amino ou cyano ; R<2> représente alkyle C1-C4 éventuellement substitué, alkényle C3-C4 éventuellement substitué ou amino cyclique substitué de 4 à 6 éléments ; R<3> représente phényle substitué ; R<4> représente alkoxycarbonyle C1-C4 éventuellement substitué, 1,3,2-phosphorinan-2-yl ou 5,5-diméthyl-1,3,2-phosphorinan-2-yl et R<5> représente alkyle C1-C4.

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