Salts of the CGRP antagonist BIBN4096 and inhalable powdered medicaments containing them

Abstract

The invention relates to salts of the active substance base 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 [BIBN4096] of formula I, the preparation thereof, a process for preparing an inhalation powder containing a salt of the active substance BIBN4096 as well as the inhalation powders which can be obtained by the process.

1 . An inhalation powder containing a pharmaceutically acceptable acid addition salt of 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, wherein the salt is in the form of spherically nanostructured particles, and wherein: 
 (a) the particles have a specific surface of between 1 m 2 /g and 20 m 2 /g,    (b) the characteristic value Q (5.8)  is between 50% and 100% and    (c) the parameter X 50  is between 1 μm and 6 μm.    
     
     
         2 . An inhalation powder according to  claim 1 , wherein the particles have a specific surface of between 1 m 2 /g and 10 m 2 /g.