Spray-dried amorphous bibn 4096 method for production and...

Details Spray-dried amorphous bibn 4096 method for production and... Spray-dried amorphous bibn 4096 method for production and...

A - Human Necessities

61

K

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

Patent

CA 2536047

The invention relates to 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), or the physiologically-acceptable salts thereof, which are stable in the amorphous state under normal conditions (T < 50 ·C, relative humidity < 75%) in the form of microparticles, methods for production of microparticles of said substances and the use of said microparticles for the production of a medicament in the application form of a powder inhalant for pulmonary and nasal inhalation, in particular, for the production of a medicament for the treatment of headaches, migraines and cluster headaches.

La présente invention concerne l'antagoniste de 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-pipéridinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-pipérazine (A) ou des sels physiologiquement acceptables dudit composé, qui sont stables à l'état amorphe dans des conditions normales (T < 50·C, humidité relative < 75%) et se présentent sous forme de microparticules. La présente invention concerne également des procédés de production de microparticules à partir de ces composés ainsi que l'utilisation de ces particules pour la fabrication d'un médicament destiné à être administré sous forme de poudre à inhaler pour l'inhalation pulmonaire et nasale, en particulier pour la fabrication d'un médicament destiné à traiter les céphalées, la migraine et l'algie vasculaire de la face.

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