Inhalative powder formulations containing the CGRP-antagonist 1 [N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine
AssigneeBoehringer Ingelheim International GmbH
InventorMichael Trunk
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Abstract
Powdered preparations for pulmonary or nasal inhalation, containing the CGRP antagonist 1-[N2-[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 a pharmaceutically acceptable salt thereof, processes for preparing them and the use thereof for preparing a pharmaceutical composition for the treatment of headaches, migraine and cluster headache.
Claims17
An inhalable powder for administration by pulmonary or nasal inhalation, containing as active substance the CGRP antagonist 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine
- or a physiologically acceptable salt thereof and an inert, homogeneous excipient, characterised in that
- (a) the parameter X50 for the particle size of the active substance is in the range from 1 μm to 6 μm, preferably from 1 μm to 3.5 μm, and
- (b) the characteristic value Q(5.8) for the active substance is at least 60%.
A process for preparing an inhalable powder for administration by pulmonary or nasal inhalation, containing as active substance the CGRP antagonist 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine
- or a physiologically acceptable salt thereof and an inert, homogeneous excipient,
- characterised in that
- (b) the active substance is micronised,
- (b) the micronised active substance is conditioned,
- (c) suitably mixed with one or more excipients according to the invention and
- (d) the amount of the powder mixture thus obtained which is to be administered is packaged in inhalettes in single doses under specified ambient climatic conditions.
Dependencies are inferred from the claim text.