Liquid pharmaceutical formulations of palonosetron

Abstract

The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.

1 - 58 . (canceled) 
     
     
         59 . An oral solution comprising:
 a) from 0.03 mg/ml to 0.2 mg/ml palonosetron or a pharmaceutically acceptable salt thereof, based on the weight of the free base;   b) from 100 mg/ml to 250 mg/ml of a sweetener;   c) from 0.005 to 1.0 mg/ml of a chelating agent; and   d) an acceptable buffer at a pH from 4.0 to 6.0.   
     
     
         60 . The oral solution of  claim 59 , comprising 0.05 mg/ml of the palonosetron or pharmaceutically acceptable salt thereof, based on the weight of the free base. 
     
     
         61 . The oral solution of  claim 59 , comprising palonosetron hydrochloride. 
     
     
         62 . The oral solution of  claim 59 , comprising 150 mg/ml of the sweetener. 
     
     
         63 . The oral solution of  claim 59 , wherein the sweetener is mannitol. 
     
     
         64 . The oral solution of  claim 59 , comprising 0.3 to 0.7 mg/ml of the chelating agent. 
     
     
         65 . The oral solution of  claim 64 , comprising 0.5 mg/ml of the chelating agent. 
     
     
         66 . The oral solution of  claim 59 , wherein the chelating agent is EDTA. 
     
     
         67 . The oral solution of  claim 59 , wherein the buffer is a citrate buffer. 
     
     
         68 . The oral solution of  claim 67 , comprising from 10 to 100 millimoles of the citrate buffer. 
     
     
         69 . The oral solution of  claim 68 , comprising from 10 to 40 millimoles of the citrate buffer. 
     
     
         70 . The oral solution of  claim 59 , wherein the pH is from 4.5 to 5.5. 
     
     
         71 . The oral solution of  claim 70 , wherein the pH is 5.0. 
     
     
         72 . A pharmaceutically stable oral solution for reducing emesis or reducing the likelihood of emesis comprising:
 a) 0.05 mg/ml palonosetron hydrochloride;   b) 150 mg/ml mannitol;   c) 0.5 mg/ml EDTA; and   d) a citric acid buffer at a pH from 5.0±0.5.