Liquid pharmaceutical formulations of palonosetron
View Patent ↗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. A pharmaceutically stable intravenous solution for reducing emesis or reducing the likelihood of emesis comprising:
a) from 0.03 mg/ml to 0.2 mg/ml palonosetron or a pharmaceutically acceptable salt thereof, buffered at a pH of from 4.0 to 6.0; and
b) a pharmaceutically acceptable sterile aqueous carrier including a tonicifying effective amount of mannitol and from 0.005 mg/ml to 1.0 mg/ml EDTA.
2. The solution of claim 1 wherein the palonosetron or pharmaceutically acceptable salt thereof is in concentration of about 0.05 mg/ml.
3. The solution of claim 1 comprising palonosetron hydrochloride.
4. The solution of claim 1 wherein the pH is from 4.5 to 5.5.
5. The solution of claim 1 wherein the pharmaceutically acceptable carrier comprises from 10 to 100 millimoles of a citrate buffer.
6. The solution of claim 1 comprising 0.3 to 0.7 mg/ml EDTA, and from 10 to 40 millimoles of a citrate buffer.
7. The solution of claim 1 comprising 0.3 to 0.7 mg/ml EDTA, from 10.0 to 80.0 mg/ml mannitol, and from 10 to 40 millimoles of a citrate buffer.
8. A pharmaceutically stable isotonic intravenous solution for reducing emesis or reducing the likelihood of emesis comprising:
a) from 0.01 mg/ml to 5 mg/ml palonosetron or a pharmaceutically acceptable salt thereof, at a pH of from 4.0 to 6.0; and
b) an aqueous pharmaceutically acceptable carrier including a chelating agent.
9. The solution of claim 8 wherein the palonosetron or pharmaceutically acceptable salt thereof is in concentration of about 0.05 mg/ml.
10. The solution of claim 8 comprising palonosetron hydrochloride.
11. The solution of claim 8 wherein the pH is from 4.5 to 5.5.
12. The solution of claim 8 wherein the pharmaceutically acceptable carrier comprises from 0.005 mg/ml to 1.0 mg/ml EDTA.
13. The solution of claim 8 wherein the pharmaceutically acceptable carrier comprises mannitol.
14. The solution of claim 8 adapted for intravenous administration.