Formulations for parenteral delivery of compounds and uses thereof
AssigneeWyeth
InventorsSyed M. Shah, Christian Ofslager, Mahdi B. Fawzi, Nataliya Bazhina
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Abstract
The present invention provides formulations that achieve effective delivery of methylnaltrexone compositions. The provided formulations are useful for preventing, treating delaying, diminishing or reducing the severity of side effects resulting from use of analgesic opioids.
Claims19
A pharmaceutical composition comprising an effective amount of methylnaltrexone or a pharmaceutically acceptable salt thereof, about 0.4 mg/mL of calcium ethylenediaminetetraacetic acid (EDTA) disodium, and about 0.1 mg/mL to about 0.8 mg/mL of glycine in an aqueous solution, wherein the solution has a pH of about 3 to 4.
A method of preparing a methylnaltrexone formulation for parenteral administration, the method comprising the steps of:
- mixing calcium EDTA, or a calcium salt EDTA derivative, and glycine with a solution of methylnaltrexone, or a pharmaceutically acceptable salt thereof;
- adjusting the pH to about 3.0 to about 4.0;
- and
- sterilizing the resulting solution, thereby preparing the methylnaltrexone formulation, wherein the formulation comprises about 0.2 mg/mL to about 0.8 mg/mL of calcium EDTA, or a calcium EDTA derivative, and about 0.1 mg/mL to about 0.8 mg/mL of glycine.
Dependencies are inferred from the claim text.