Compositions containing opioid antagonists, particularly alvimopan and its active metabolite, with improved solubility and bioavailability for oral or parenteral administration, injectable dosage formulations, kits, and methods of making and using same are disclosed. In preferred embodiments, invention provides injectable formulations containing opioid antagonists, particularly alvimopan and its active metabolite, having low solubility that may be readily prepared, are stable during storage, and...

The present invention provides a novel process for the purification of alvimopan. In accordance with the present invention alvimopan was dissolved in dimethylformamide and heated to 120 to 125 deg C and then added n-butanol at room temperature the contents were stirred for 15 hours filtered and then dried to obtain pure alvimopan.

The present invention provides a novel process for the purification of alvimopan. In accordance with the present invention alvimopan was dissolved in dimethylformamide and heated to 120 to 125 deg C, and then added n-butanol at room temperature, the contents were stirred for 15 hours, filtered and then dried to obtain pure alvimopan.

Compositions containing opioid antagonists, particularly alvimopan and its active metabolite, with improved solubility and bioavailability for oral or parenteral administration, injectable dosage formulations, kits, and methods of making and using same are disclosed. In preferred embodiments, invention provides injectable formulations containing opioid antagonists, particularly alvimopan and its active metabolite, having low solubility that may be readily prepared, are stable during storage, and...