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