Amorphous Aprepitant Coprecipitates
A coprecipitate comprising amorphous aprepitant and a pharmaceutically acceptable carrier is prepared by rapidly removing solvent from a solution containing aprepitant and the carrier.
1 . A coprecipitate comprising amorphous aprepitant and a pharmaceutically acceptable carrier.
2 . The coprecipitate of claim 1 , which is in the form of a molecular dispersion.
3 . The coprecipitate of either of claims 1 , wherein a pharmaceutically acceptable carrier comprises polyvinylpyrrolidone.
4 . The coprecipitate of claim 1 , prepared by removing solvent from a solution comprising aprepitant and a pharmaceutically acceptable carrier.
5 . The coprecipitate of claim 1 , prepared by removing solvent from a solution comprising aprepitant and a pharmaceutically acceptable carrier, under reduced pressure.
6 . The coprecipitate of claim 1 , having an aqueous solubility at least about 0.25 mg/ml.
7 . The coprecipitate of claim 1 , having an aqueous solubility at least about 0.5 mg/ml.
8 . The coprecipitate of claim 1 , having an aqueous solubility at least about 1 mg/ml.
9 . The coprecipitate of claim 3 , having an aqueous solubility at least about 1 mg/ml.
10 . The coprecipitate of claim 1 , in which no discrete zones of amorphous aprepitant and of pharmaceutically acceptable carrier can be observed in a particle.
11 . A process for preparing a coprecipitate of amorphous aprepitant and a pharmaceutically acceptable carrier, comprising:
a) providing a solution containing aprepitant and a pharmaceutically acceptable carrier;
b) removing solvent to form a solid; and
c) optionally, drying a formed solid.
12 . The process of claim 11 , wherein solvent is removed in b) at temperatures about 20° C. to about 70° C.
13 . The process of claim 11 , wherein solvent is removed in b) under a vacuum.
14 . The process of claim 11 , wherein solvent is removed in b) using a technique comprising spray drying or agitated thin film drying.
15 . A coprecipitate of amorphous aprepitant and a pharmaceutically acceptable carrier, prepared by a process of claim 11 .
16 . A coprecipitate comprising amorphous aprepitant and polyvinylpyrrolidone, in the form of a molecular dispersion.
17 . The coprecipitate of claim 16 , having an aqueous solubility at least about 0.25 mg/ml.
18 . The coprecipitate of claim 16 , having an aqueous solubility at least about 0.5 mg/ml.
19 . The coprecipitate of claim 16 , having an aqueous solubility at least about 1 mg/ml.
20 . The coprecipitate of claim 16 , in which no discrete zones of amorphous aprepitant and of polyvinylpyrrolidone can be observed in a particle.
21 . A coprecipitate of amorphous aprepitant and a pharmaceutically acceptable carrier, prepared by a process of claim 12 .
22 . A coprecipitate of amorphous aprepitant and a pharmaceutically acceptable carrier, prepared by a process of claim 13 .
23 . A coprecipitate of amorphous aprepitant and a pharmaceutically acceptable carrier, prepared by a process of claim 14 .