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Claims for Patent: 5,380,922

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Claims for Patent: 5,380,922

Title: Benzenedimethanol suitable for micronisation
Abstract:1-Hydroxy-2-naphthalene carboxylate (hydroxynaphthoate) salt of 4-hydroxy-a.sup.1 -[[[6-(4-phenylbutoxy)hexyl]-amino]methyl]-1,3-benzendimethanol in the form of spherical accretions of microcrystals, the spherical accretions being free-flowing, friable and micronisable and preferably having a mean particle size of from 70 to 300 mm and a mean surface area from 4 to 12 m.sup.2 g.sup.-1. The hydroxynaphthoate salt in the claimed form may be prepared by quenching a hot organic/aqueous organic solution containing the salt with a cold organic/aqueous organic solvent.
Inventor(s): Beach; Steven F. (Ware, GB3), Latham; David W. S. (Ware, GB3), Roberts; Tony G. (Ware, GB3), Sidgwick; Colin B. (Ware, GB3)
Assignee: Glaxo Group Limited (London, GB2)
Application Number:08/050,298
Patent Claims: 1. 1-Hydroxy-2-naphthalenecarboxylate salt of 4-hydroxy-.alpha..sup.1 -[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol in the form of spherical accretions of microcrystals, the spherical accretions being free-flowing, friable and micronisable.

2. The hydroxynaphthoate salt according to claim 1 wherein the spherical accretions of microcrystals have a mean particle size from 70 to 300 .mu.m.

3. The hydroxynaphthoate salt according to claim 1 wherein the spherical accretions of microcrystals have a mean surface area from 4 to 12 m.sup.2 g.sup.-1.

4. The hydroxynaphthoate salt according to claim 1 wherein the spherical accretions of microcrystals have a particle size distribution from 100 to 1000 .mu.m.

5. The hydroxynaphthoate salt according to claim 1 wherein the spherical accretions of microcrystals have an aerated bulk density from 0.2 to 0.5 gml.sup.-1.

6. The hydroxynaphthoate salt according to claim 1 wherein the spherical accretions of microcrystals have a cohesivity from 0 to 20%.

7. The hydroxynaphthoate salt according to claim 1 wherein the spherical accretions of microcrystals have a uniformity coefficient from 1 to 5.

8. The hydroxynaphthoate salt according to claim 1 wherein the spherical accretions of microcrystals have an angle of repose from 25.degree. to 50.degree..

9. The hydroxynaphthoate salt according to claim 1 wherein the spherical accretions of microcrystals have a compressibility from 5 to 25%.

10. The hydroxynaphthoate salt according to claim 1 wherein the spherical accretions of microcrystals each comprise thin crystalline plates arranged radially about a central core or void.

11. A process for the micronisation of the 1-hydroxy-2-naphthalenecarboxylate salt of 4-hydroxy-.alpha..sup.-1 -[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol comprising feeding the hydroxynaphthoate salt of 4-hydroxy-.alpha..sup.-1 [[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3benzendimethanol in the form of spherical accretions of microcrystals, the spherical accretions being free-flowing, friable and micronisable, into a microniser, micronising the hydroxynaphthoate salt to give micronised material and collecting the micronised material.

12. A process for the preparation of the 1 -hydroxy-2-naphthalenecarboxylate salt of 4-hydroxy-.alpha..sup.1 -[[[6-(4-phenylbutoxy)hexyl]amino]methyl]- 1,3-benzendimethanol in the form of spherical accretions of microcrystals, the spherical accretions being free-flowing, friable and micronisable said process comprising quenching a hot organic or hot aqueous organic solution of the hydroxynaphthoate salt wit a cold organic or cold aqueous organic solvent to give spherical accretions of microcrystals of the hydroxynaphthoate salt and collecting said spherical accretions of microcrystals.

13. A process according to claim 12 wherein a hot organic solution of hydroxynaphthoate salt is quenched with a cold organic solvent to give spherical accretions of microcrystals of the hydroxynaphthoate salt.

14. A process according to claim 12 wherein the organic solvent employed in the hot organic or hot aqueous solution has a boiling point (at 760 mm Hg) from 40.degree. to 150.degree. C.

15. A process according to claim 14 wherein the organic solvent comprises a lower (C.sub.1-4)alkyl alcohol, a lower (C.sub.1-4) alkyl ether or a lower (C.sub.1-4) alkyl ester.

16. A process according to claim 15 wherein the organic solvent comprises a lower alkyl alcohol.

17. A process according to claim 12 wherein the organic solvent employed in the cold organic or cold aqueous organic solvent has a freezing point from -150.degree. to -20.degree. C.

18. A process according to claim 17 wherein the organic solvent comprises a lower (C.sub.1-4) alkyl alcohol, a lower (C.sub.1-4) alkyl ether or a lower (C.sub.1-4) alkyl ester.

19. A process according to claim 18 wherein the organic solvent comprises a lower alkyl alcohol.

20. A process according to claim 12 wherein the temperature of the hot organic or the hot aqueous solution is from 30.degree. to 80.degree. C.

21. A process according to claim 12 wherein the temperature of the cold organic or the cold aqueous solvent is from -35.degree. to +15.degree. C.

22. A process according to claim 12 wherein during the quenching of the hot organic or hot aqueous organic solution of the hydroxynaphthoate salt with the cold organic or cold aqueous organic solvent, the temperature of the mixture is maintained at a temperature below about +20.degree. C.

23. A process according to claim 12 wherein the hot organic or hot aqueous solution of the hydroxynaphthoate salt is prepared by mixing 1-hydroxy-2-naphthoic acid and4-hydroxy-.alpha..sup.1 -[[[6-(4-phenylbutoxy)hexyl]amino]methyl-1,3-benzenedimethanolin ahot organic or hot aqueous organic solvent.

24. The salt according to claim 2 wherein the mean particle size is from 100 to 200 .mu.m.

25. The salt according to claim 3 wherein the mean surface area is from 6 to 10 m.sup.2 g.sup.-1.

26. The salt according to claim 15 wherein the aerated bulk density is from 0.3 to 0.4 gml.sup.-1.

27. The salt according to claim 6 wherein the cohesivity is from 0 to 5%.

28. The salt according to claim 7 wherein the uniformity coefficient is about 3.

29. The salt according to claim 8 wherein the angle of repose is from 40.degree. to 50.degree..

30. The salt according to claim 9 wherein the compressibility is from 8 to 20%.

31. A process according to claim 14 wherein the boiling point is from 60.degree. to 120.degree. C.

32. A process according to claim 16 wherein the organic solvent comprises methanol, ethanol or isopropanol.

33. A process according to claim 32 wherein the organic solvent comprises methanol.

34. A process according to claim 17 wherein the freezing point is from -130.degree. to -150.degree. C.

35. A process according to claim 19 wherein the organic solvent comprises methanol, ethanol, or isopropanol.

36. A process according to claim 35 wherein the organic solvent comprises isopropanol.

37. A process according to claim 20 wherein the temperature is from 40.degree. to 70.degree. C.

38. A process according to claim 21 wherein the temperature is from -25.degree. to +10.degree. C.

39. A process according to claim 22 wherein the temperature is from -10.degree. to +20.degree. C.
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