Stable pharmaceutical formulations of methylnaltrexone
Stable pharmaceutical compositions useful for administering methylnaltrexone are described, as are methods for making the same. Kits, including these pharmaceutical compositions, also are provided.
1. A stable pharmaceutical preparation comprising a solution of methylnaltrexone or salt thereof and a chelating agent; wherein the chelating agent is ethylenediaminetriacetic acid (EDTA) or a derivative thereof.
2. The stable pharmaceutical preparation of claim 1 , wherein the preparation comprises methylnaltrexone bromide.
3. The stable pharmaceutical preparation of claim 1 , wherein the EDTA derivative is edetate calcium disodium.
4. The stable pharmaceutical preparation of claim 1 , wherein the preparation further comprises an isotonicity agent and a buffering agent.
5. The stable pharmaceutical preparation of claim 4 , wherein the isotonicity agent is sodium chloride and the buffering agent is glycine.
6. The stable pharmaceutical preparation of claim 5 , wherein the preparation is suitable for parenteral delivery.
7. The stable pharmaceutical preparation of claim 1 , wherein the preparation is delivered at a dose from about 0.01 to 1.00 mg/kg body weight per day.
8. The stable pharmaceutical preparation of claim 1 , wherein the preparation is delivered at a dose from about 0.1 to 0.3 mg/kg body weight per day.
9. A method for treating an opioid-induced peripheral side effect comprising administering to a patient the stable pharmaceutical preparation of claim 1 in an amount effective to treat the side effect.
10. The method of claim 9 , wherein the opioid induced peripheral side effect is constipation.
11. The pharmaceutical preparation of claim 1 , wherein the concentration of methylnaltrexone or salt thereof ranges from about 1.0 to about 50.0 mg/ml.
12. The pharmaceutical preparation of claim 1 , wherein the concentration of methylnaltrexone or salt thereof is about 20 mg/ml.
13. The pharmaceutical preparation of claim 1 , wherein the concentration of chelating agent ranges from about 0.1 to about 25.0 mg/ml.
14. The pharmaceutical preparation of claim 1 , wherein the concentration of chelating agent ranges from about 0.1 to about 2.5 mg/ml.
15. The pharmaceutical preparation of claim 1 , wherein the methylnaltrexone or salt thereof is methylnaltrexone bromide and is at a concentration of about 20 mg/mL, and wherein the EDTA or a derivative thereof is at a concentration of about 0.1 to about 2.5 mg/ml.