STORAGE-STABLE READY-TO-USE INJECTABLE FORMULATIONS OF FOSAPREPITANT DIMEGLUMINE
The present application provides a stable, ready-to-use fosaprepitant dimeglumine formulation which is easy to administer without need of any reconstitution step and has a desirable solubility, stability and safety profile. The concentration of the fosaprepitant dimeglumine in the liquid formulation is preferably less than about 80 mg/ml, or more preferably between about 20 mg/ml to about 60 mg/ml. In certain embodiments, the liquid formulation retains at least about 90% chemical stability of the fosaprepitant dimeglumine after storage for a commercially reasonable amount of time at a temperature between about 0° C. to about 40° C.
1 . A storage-stable liquid formulation comprising fosaprepitant dimeglumine and a pharmaceutically acceptable vehicle.
2 . The storage-stable liquid formulation of claim 1 , wherein a concentration of the fosaprepitant dimeglumine in the liquid formulation is less than about 80 mg/ml.
3 . The storage-stable liquid formulation of claim 1 , wherein a concentration of the fosaprepitant dimeglumine in the liquid formulation is between about 20 mg/ml to about 60 mg/ml.
4 . The storage-stable liquid formulation of claim 1 , wherein the liquid formulation retains at least about 90% chemical stability of the fosaprepitant dimeglumine after storage for about six months at a temperature between about 0° C. to about 40° C.
5 . The storage-stable liquid formulation of claim 1 , wherein the vehicle comprise an NaCl solution, a concentration of the fosaprepitant dimeglumine in the liquid formulation is between about 20 mg/ml to about 60 mg/ml, and a chemical stability of the fosaprepitant dimeglumine after storage of about 32 days at room temperature is greater than 95%.
6 . The storage-stable liquid formulation of claim 5 , wherein the chemical stability of the fosaprepitant dimeglumine after storage of about four months at between about 2° C. and about 8° C. is greater than 99%.
7 . The storage-stable liquid formulation of claim 5 , wherein a pH of the liquid formulation is between about 7 to about 11.5.
8 . The storage-stable liquid formulation of claim 5 , comprising propylene glycol and ethanol.
9 . The storage-stable liquid formulation of claim 8 , wherein the propylene glycol and ethanol are present in the liquid formulation at a ratio of about 2.5:2.0.
10 . The storage-stable liquid formulation of claim 8 , wherein the propylene glycol and ethanol are present in the liquid formulation at a ratio of about 2.5:1.5.
11 . The storage-stable liquid formulation of claim 8 , wherein the propylene glycol and ethanol are present in the liquid formulation at a ratio between about 2.5:2.0 and about 2.5:1.5.
12 . The storage-stable liquid formulation of claim 5 , wherein the NaCl solution has a concentration of about 0.9%.
13 . The storage-stable liquid formulation of claim 1 , wherein the vehicle comprise an NaCl solution, a concentration of the fosaprepitant dimeglumine in the liquid formulation is between about 20 mg/ml to about 60 mg/ml, and a stability of the fosaprepitant dimeglumine after storage of about 29 days at room temperature is at least 96%.
14 . The storage-stable liquid formulation of claim 13 , comprising propylene glycol and wherein the propylene glycol and NaCl solution are present at a ratio of about 1:1.
15 . The storage-stable liquid formulation of claim 13 , comprising ethanol and wherein the ethanol and NaCl solution are present at a ratio of about 1:1.
16 . The storage-stable liquid formulation of claim 13 , wherein the stability of the fosaprepitant dimeglumine after storage of about 43 days at room temperature is at least 96%.
17 . The storage-stable liquid formulation of claim 1 , wherein the fosaprepitant dimeglumine is at least one of a pharmaceutically acceptable salt, solvate, hydrate, or a n anhydrous form thereof.
18 . The storage-stable liquid formulation of claim 1 , wherein the liquid formulation is one of a solution, suspension, or an emulsion.