Amorphous eprosartan mesylate and process for the preparation thereof
Eprosartan mesylate substantially in an amorphous form is disclosed. A composition comprising eprosartan mesylate in a solid form, wherein at least about 80% by weight of the solid eprosartan mesylate is in an amorphous form is also disclosed. The present invention also provides a process for preparing eprosartan mesylate substantially in an amorphous form by providing a solution of eprosartan mesylate in one or more solvents capable of dissolving the eprosartan mesylate and substantially removing the solvent from the solution.
1 . Eprosartan mesylate in an amorphous form.
2 . A composition comprising eprosartan mesylate in a solid form, wherein at least about 80% by weight of the solid is eprosartan mesylate in an amorphous form.
3 . The composition of claim 2 , wherein the amorphous eprosartan mesylate has a chemical purity of at least about 96%.
4 . The composition of claim 2 , wherein the amorphous eprosartan mesylate has a chemical purity of at least about 99%.
5 . The composition of claim 2 , wherein the amorphous eprosartan mesylate has a chemical purity of at least about 99.5%.
6 . The composition of claim 2 , wherein the eprosartan mesylate has a D 50 particle size of less than about 300 microns.
7 . The composition of claim 2 , wherein the eprosartan mesylate has a D 50 particle size of less than about 50 microns.
8 . The composition of claim 2 , wherein the eprosartan mesylate has a D 50 particle size less than about 10 microns.
9 . The composition of claim 2 , wherein the eprosartan mesylate has a D 90 particle size of less than about 300 microns.
10 . The composition of claim 2 , wherein the eprosartan mesylate has a D 90 particle size of less than about 50 microns.
11 . The composition of claim 2 , wherein the eprosartan mesylate has a D 90 particle size less than about 10 microns.
12 . The composition of claim 2 , wherein the amorphous eprosartan mesylate has an average particle size less than about 500 nm.
13 . The composition of claim 2 , wherein the amorphous eprosartan mesylate has an average particle size less than about 400 nm.
14 . The composition of claim 2 , wherein the amorphous eprosartan mesylate has an average particle size less than about 250 nm.
15 . The composition of claim 12 , in the form of a high drug load tablet.
16 . A pharmaceutical composition comprising a therapeutically effective amount of the eprosartan mesylate in an amorphous form of claim 1 and at least one pharmaceutically acceptable excipient.
17 . A pharmaceutical composition comprising a therapeutically effective amount of the composition of claim 2 and at least one pharmaceutically acceptable excipient.
18 . A process for preparing eprosartan mesylate substantially in an amorphous form, the process comprising:
(a) providing a solution of eprosartan mesylate in one or more solvents capable of dissolving the eprosartan mesylate; and
(b) substantially removing the solvent from the solution to provide amorphous eprosartan mesylate.
19 . The process of claim 18 , wherein step (b) comprises spray drying.
20 . The process of claim 18 , 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.