Pharmaceutical compositions based on azetidine derivatives

Details Pharmaceutical compositions based on azetidine derivatives Pharmaceutical compositions based on azetidine derivatives

A - Human Necessities

61

K

A61K 47/14 (2006.01) A61K 9/48 (2006.01) A61K 31/137 (2006.01) A61K 31/397 (2006.01) A61K 45/06 (2006.01)

Patent

CA 2470443

The invention concerns a stable pharmaceutical composition comprising at least an azetidine derivative of general formula (Ia) or (Ib), wherein: Ar is aromatic or heteroaromatic group optionally substituted by one or several C¿1?-C¿4? alkyl, halogen, NO¿2?, CN, C¿1?-C¿4? alkoxy or OH, optionally combined with another active principle capable of potentiating the effects of the azetidine derivative of general formula (Ia) or (Ib), in a system comprising not more than two main excipients selected among a non-ionic surfactant with hydrophilic character capable of solubilizing the azetidine derivative of general formula (Ia) or (Ib) and optionally the active principle potentiating the effects of the azetidine derivative, and capable of causing the formation of a colloidal system, optionally with addition of a second lipophilic excipient, stabilizing the formulation. The pharmaceutical compositions comprising azetidine derivatives of formulae (Ia) or (Ib) are particularly useful because of the high affinity of said derivatives for cannabinoid receptors.

Composition pharmaceutique stable comprenant au moins un dérivé d'azétidine de formule générale (Ia) ou (Ib) dans laquelle Ar est un groupement aromatique ou hétéroaromatique éventuellement substitué par un ou plusieurs (C1-C4)alkyle, halogène, NO2, CN, (C1-C4)alkoxy ou OH, éventuellement en association avec un autre principe actif capable de potentialiser les effets du dérivé d'azétidine de formule générale (Ia) ou (Ib), dans un système comprenant au plus 2 excipients principaux choisis parmi un agent tensio-actif non-ionique à caractère hydrophile capable de solubiliser le dérivé d'azétidine de formule générale (Ia) ou (Ib) et le cas échéant le principe actif potentialisant les effets du dérivé d'azétidine, et capable de provoquer la formation d'un système colloïdal, additionné éventuellement d'un second excipient de nature lipophile, stabilisant la formulation.Les compositions pharmaceutiques comprenant des dérivés d'azétidine de formules (Ia) ou (Ib) sont particulièrement intéressantes du fait de la forte affinité de ces dérivés pour les récepteurs cannabinoïdes.

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