Crystalline Micronisate, Process for the Manufacture Thereof and Use Thereof for the Preparation of a Medicament
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Abstract
The invention relates to a crystalline micronisate of (1 α,2β,4β,5α,7β)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane-bromide, processes for preparing it and its use for preparing a pharmaceutical composition, particularly for preparing a pharmaceutical composition with an anticholinergic activity.
41 Citations
18 Claims
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1-9. -9. (canceled)
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10. A pharmaceutical composition, comprising crystalline tiotropium bromide micronisate characterised by a particle size X50 of between 1.0 μ
- m and 3.5 μ
m at a Q5.8) value of more than 60%, by a specific surface value in the range between 2 m2/g and 5 m2/g, by a specific heat of solution of more than 65 Ws/g and by a water content from about 1% to about 4.5%, wherein the crystalline tiotropium bromide micronisate is obtained from crystalline tiotropium bromide monohydrate, which crystalline tiotropium bromide monohydrate when thermally analysed by DSC has an endothermic maximum at 230±
5°
C. at a heating rate of 10K/min, has an IR spectrum which has bands inter alia at wavelengths 3570, 3410, 3105, 1730, 1260, 1035 and 720 cm−
1 and which is characterised by a simple monoclinic cell with the following dimensions;
a=18.0774 Å
, b=11.9711 Å
, c=9.9321 Å
, β
=102.691°
, V =2096.96 Å
3;
in admixture with at least one physiologically acceptable excipient. - View Dependent Claims (11, 12, 13, 14, 15, 16, 17, 18)
- m and 3.5 μ
Specification