Powder formulation comprising the cgrp antagonist...

A - Human Necessities – 61 – K

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Details

A61K 31/517 (2006.01) A61K 9/12 (2006.01) A61K 9/72 (2006.01)

Patent

CA 2536053

The invention relates to a powder inhalant for pulmonary or nasal inhalation, comprising the CGRP antagonist 1-[N?2¿-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine (A) in the form of spherical, nano-structured microparticles, which are stable in the amorphous state under normal conditions (T < 50 ·C, relative humidity < 75%), a method for production of said microparticles and the use thereof for the production of the powder inhalant for the treatment of headaches, migraines and cluster headaches.

La présente invention concerne une substance à inhaler pulvérulente pour l'inhalation pulmonaire ou nasale qui contient l'antagoniste CGRP 1[<I>N</I>?2¿-[3,5-dibromo-<I>N</I>-[[4-(3,4-dihydro-2(1<I>H</I>)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-pipérazine (A) sous forme de microparticules sphériques nanostructurées qui sont stables à l'état amorphe dans des conditions normales (T < 50 ·C, humidité relative < 75%). La présente invention concerne également un procédé de production de ces microparticules ainsi que leur utilisation pour fabriquer ladite substance pulvérulente destinée à traiter les céphalées, la migraine et l'algie vasculaire de la face.

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