Amorphous frovatriptan succinate and process for the preparation thereof
Frovatriptan succinate substantially in an amorphous form is disclosed. Also disclosed is a composition comprising frovatriptan succinate in a solid form, wherein at least about 80% by weight of the solid is frovatriptan succinate in an amorphous form. The present invention also provides a process for preparing frovatriptan succinate substantially in an amorphous form by providing a solution of frovatriptan succinate in one or more solvents capable of dissolving the frovatriptan succinate and substantially removing the solvent from the solution.
1 . Frovatriptan succinate in an amorphous form.
2 . A composition comprising frovatriptan succinate in a solid form, wherein at least about 80% by weight of the solid is frovatriptan succinate in an amorphous form.
3 . The composition of claim 2 , wherein the frovatriptan succinate has a chemical purity of about 96%.
4 . The composition of claim 2 , wherein the frovatriptan succinate has a chemical purity of about 99%.
5 . The composition of claim 2 , wherein the frovatriptan succinate has a chemical purity of about 99.5%.
6 . The composition of claim 2 , wherein the frovatriptan succinate has a D 50 particle size of less than about 300 microns.
7 . The composition of claim 2 , wherein the frovatriptan succinate has a D 50 particle size of less than about 200 microns.
8 . The composition of claim 2 , wherein the frovatriptan succinate has a D 50 particle size of less than about 150 microns.
9 . The composition of claim 2 , wherein the frovatriptan succinate has a D 50 particle size less than about 50 microns.
10 . The composition of claim 2 , wherein the frovatriptan succinate has a D 50 particle size less than about 10 microns.
11 . The composition of claim 2 , wherein the frovatriptan succinate has a D 90 particle size of less than about 300 microns.
12 . The composition of claim 2 , wherein the frovatriptan succinate has a D 90 particle size of less than about 200 microns.
13 . The composition of claim 2 , wherein the frovatriptan succinate has a D 90 particle size of less than about 150 microns.
14 . The composition of claim 2 , wherein the frovatriptan succinate has a D 90 particle size less than about 50 microns.
15 . The composition of claim 2 , wherein the frovatriptan succinate has a D 90 particle size less than about 10 microns.
16 . A pharmaceutical composition comprising a therapeutically effective amount of the frovatriptan succinate in an amorphous form of claim 1 and at least one pharmaceutical excipient.
17 . A pharmaceutical composition comprising a therapeutically effective amount of the composition of claim 2 and at least one pharmaceutical excipient.
18 . A pharmaceutical composition comprising a therapeutically effective amount of the composition of claim 3 and at least one pharmaceutical excipient.
19 . A process for preparing frovatriptan succinate substantially in an amorphous form, the process comprising:
(a) providing a solution of frovatriptan succinate in one or more solvents capable of dissolving the frovatriptan succinate; and
(b) substantially removing the solvent from the solution to provide amorphous frovatriptan succinate.
20 . The process of claim 19 , wherein the solvents are selected from the group consisting of an alcoholic solvent having from 1 to 6 carbon atoms, aromatic solvent, non-aromatic solvent and combinations thereof.