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Claims for Patent: 7,309,707

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Claims for Patent: 7,309,707

Title:Crystalline micronisate, process for the manufacture thereof and use thereof for the preparation of a medicament
Abstract:The invention relates to a crystalline micronisate of (1.alpha.,2.beta.,4.beta.,5.alpha.,7.beta.)-7-[(hydroxydi-2-thienylacetyl- )oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0.sup.2,4]nonane-bromide, processes for preparing it and its use for preparing a pharmaceutical composition, particularly for preparing a pharmaceutical composition with an anticholinergic activity.
Inventor(s): Bender; Helmut (Wiesbaden, DE), Graebner; Hagen (Ingelheim, DE), Schindler; Konrad (Ingelheim, DE), Trunk; Michael (Ingelheim, DE), Walz; Michael (Bingen, DE)
Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG (Ingelheim, DE)
Application Number:10/385,175
Patent Claims: 1. Crystalline tiotropium bromide micronisate, characterised by a particle size X.sub.50 of between 1.0 .mu.m and 3.5 .mu.m at a Q.sub.(5.8) value of more than 60%, by a specific surface value in the range between 2 m.sup.2/g and 5 m.sup.2/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.degree. 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.sup.-1 and which is characterised by a simple monoclinic cell with the following dimensions: a=18.0774 .ANG., b=11.9711 .ANG., c=9.9321 .ANG., .beta.=102.691.degree., V=2096.96 .ANG..sup.3.

2. The crystalline tiotropium bromide micronisate according to claim 1, characterised in that the particle size X.sub.50 has a value of 1.1 .mu.m to 3.3 .mu.m, at a Q.sub.(5.8) value of more than 70%.

3. The crystalline tiotropium bromide micronisate according to one of claims 1 or 2, characterised in that it has a specific surface value in the range from 2.5 m.sup.2/g to 4.5 m.sup.2/g.

4. The crystalline tiotropium bromide micronisate according claim 1, characterised by a specific heat of solution of more than 71 Ws/g.

5. The crystalline tiotropium bromide micronisate according to claim 1, characterised by a water content from about 1.4% to about 4.2%.

6. A process for preparing crystalline tiotropium bromide micronisate which comprises the steps of: a) obtaining crystalline tiotropium bromide monohydrate, which crystalline tiotropium bromide monohydrate when thermally analysed by DSC has an endothermic maximum at 230.+-.5.degree. C. at a heating rate of 10K/min, has bands inter alia at wavelengths 3570, 3410, 3105, 1730, 1260, 1035 and 720 cm.sup.-1 and which is characterised by a simple monoclinic cell with the following dimensions: a=18.0774 .ANG., b=11.9711 .ANG., c=9.9321 .ANG., .beta.=102.691.degree., V=2096.96 .ANG..sup.3, b) micronizing the crystalline tiotropium bromide monohydrate so obtained and, c) exposing the resulting micronized crystalline tiotropium bromide at a temperature of about 15 to about 40.degree. C. to water with a relative humidity of at least about 40% for a period of at least about 6 hours.

7. The process according to claim 6, characterised in that the tiotropium bromide monohydrate is micronized under inert gas.

8. The process according to claim 6, characterised in that the tiotropium bromide monohydrate is micronized using an air jet mill with the following grinding parameters: TABLE-US-00014 grinding pressure: about 2 about 8 bar; feed pressure: about 2 about 8 bar; grinding gas/feed gas: nitrogen; product supply: about 5 about 35 g/min.

9. The process according to claim 8, characterised in that the micronized tiotropium bromide is exposed at a temperature of about 20--about 35.degree. C. is exposed to water vapour at a relative humidity of about 50--about 95% for a period of about 12 to 48 hours.
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